Forthcoming Papers                                                                                   Published Papers

Forthcoming Papers

Independent Papers

Latifa Douali ¹, Didier Villemin ², Abdelmajid Zyad ³ and Driss Cherqaoui ¹*
Artificial Neural Networks : Non-linear QSAR Studies of HEPT Derivatives as HIV-1 Reverse Transcriptase Inhibitors
1 Département de Chimie, Faculté des Sciences Semlalia BP 2390 Université Cadi Ayyad, Marrakech, Morocco. Fax : (+212) 44-43-74-08 
2 Ecole Nationale Supérieure d'Ingénieurs (E.N.S.I.), I. S. M. R. A., LCMT, UMR CNRS n° 6507, 6 boulevard Maréchal Juin, 14050, Caen Cedex, France.
3 Laboratoire d’Immunologie, Biochimie et Biologie Moléculaire, Faculté des Sciences et Techniques B.P. 523, Université Cadi-Ayyad, Béni-Mellal, Morocco.
* Author to whom correspondence should be addressed; E-mail : [email protected]
Received: 13 March 2003/  Accepted: 17 April 2003/

Ernesto Estrada*^{1 2}, Jose A. Quincoces ³ and Grace Patlewicz ¹
Creating Molecular Diversity from Antioxidants in Brazilian Propolis. Combination of TOPS-MODE QSAR and Virtual Structure Generation
1 Safety & Environmental Assurance Centre (SEAC), Unilever Colworth, Sharnbrook, Bedford, MK44 1LQ, UK.
2 RIAIDT, University of Santiago de Compostela, Santiago de Compostela 15706, Spain.
3 Grupo de Síntese Orgânica, Universidade Bandeirante de São Paulo, Rua Maria Cândida 1813, Vila Guilherme, CEP: 02071-013, São Paulo - SP - Brasil 
* Author to whom correspondence should be addressed; E-mail : [email protected]
Received: 3 June 2003/  Accepted: 19 June 2003/

Irving Sucholeiki*, Leticia M. Toledo-Sherman, Christopher M. Hosfield, Kelly Boutilier, Leroi V. DeSouza & David R. Stover
Novel Magnetic Supports For Small Molecule Affinity Capture Of Proteins for Use In Proteomics.
MDS Proteomics Inc., 550 Boston Avenue, 2nd Floor, Medford, MA 02155
* Author to whom correspondence should be addressed; E-mail : [email protected]
Received: 17 March 2003/  Accepted: 10 July 2003/

Linda A. Landon ¹, Jun Zou ¹, and Susan L. Deutscher ^1,2*
An Effective Combinatorial Strategy to Increase Affinity of Carbohydrate Binding by Peptides.
1. Department of Biochemistry, M121 Medical Sciences Bldg., University of Missouri, Columbia, MO 65212.
2. Harry S Truman Memorial Veterans Administration Hospital, Research Service, 800 Hospital Dr., Columbia, MO 65201-5297.
*To whom correspondence should be addressed; Telephone: 573/882-2454 or 573/882-1493, FAX: 573/884-4597. Email: [email protected]
Received: 3 May 2003/  Accepted: 22 August 2003/

Special issue on CombiChem in Spain (Guest edited by Dr. Jose I. Borrell)

José I. Borrell*
Editorial: Past, present and future of the Combinatorial Chemistry in Spain
Grup d'Enginyeria Molecular, Institut Químic de Sarrià, Universitat Ramon Llull, Via Augusta 390, E-08017 Barcelona, Spain
* Author to whom correspondence should be addressed; tel: +34-932 672 000, fax: +34-932 056 266, E-mail: [email protected]
Received: /  Accepted: /

Alfonso Cornejo,1 José M. Fraile,2 José I. García,2 María J. Gil,1 Víctor Martínez-Merino 1 and José A. Mayoral2*
Running title: Pybox immobilization
Immobilizing a single pybox ligand onto a library of solid supports
1 Dep. Química Aplicada, Universidad Pública de Navarra, E-31006 Pamplona (Spain).
2 Dep. Química Orgánica, Instituto de Ciencia de Materiales de Aragón, Universidad de Zaragoza-C.S.I.C., E-50009 Zaragoza (Spain).
* Author to whom correspondence should be addressed; Telephone and FAX: +34 976 762077. E-mail: [email protected]
Received: 28 April 2003/  Accepted: 3 June 2003/

José L. Falcó, José I. Borrell, Jordi Teixidó*
Solid-phase synthesis of 2-substituted 4-amino-7-oxo-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidines
Grup d'Enginyeria Molecular, Institut Químic de Sarrià, Universitat Ramon Llull, Via Augusta 390, E-08017 Barcelona, Spain
* Author to whom correspondence should be addressed; tel: +34-932 672 000, fax: +34-932 056 266, E-mail: [email protected]
Received:  6 May 2003/  Accepted: 10 June 2003/

M. Teresa Pastor^1† & Enrique Pérez-Payá^1,2*
Combinatorial chemistry of b-hairpins
1 Departament de Bioquímica i Biologia Molecular, Universitat de València, E-46100 Burjassot, Valencia, Spain
2 Fundación Valenciana de Investigaciones Biomédicas, CSIC. Amadeo de Saboya, 4. E-46010 Valencia, Spain
(† Present address: European Molecular Biology Laboratory, Structures and Biocomputing, Meyerhofstrasse 1, D-69117 Heidelberg, Germany)
* Author to whom correspondence should be addressed;  Tel: +34 963391258, Fax: +34 963601453, E-mail: [email protected]
Received: 12 June 2003/  Accepted: 8 July 2003/

Guillermo Gerona-Navarro,^a,b Miriam Royo^,b,c Mª Teresa García-López,^a Fernando Albericio,^b,d and Rosario González-Muñiz^a*
Exploring Solid-Phase Approaches for the Preparation of New b-Lactams from Amino Acids
a Instituto de Química Médica (CSIC), Juan de la Cierva 3, 28006 Madrid, Spain
b Department of Organic Chemistry, University of Barcelona, Martí i Franqués 1, 08028 Barcelona, Spain
c Combinatorial Chemistry Unity, Barcelona Science Park, University of Barcelona, Josep Samitier 1, 08028 Barcelona, Spain
d Barcelona Biomedical Research Institute, Barcelona Science Park, University of Barcelona, Josep Samitier 1, 08028 Barcelona, Spain
* Author to whom correspondence should be addressed;
Received: 25 April 2003/  Accepted: 9 July 2003/

Fabien Fontaine, Manuel Pastor, Hugo Gutiérrez-de-Terán, Juan J. Lozano
Use of alignment-free molecular descriptors in diversity analysis and optimal sampling of molecular libraries
Research Group on Biomedical Informatics (GRIB), IMIM, Universitat Pompeu Fabra, C/ Dr. Aiguader 80, E-08003 Barcelona, Spain.
* Author to whom correspondence should be addressed;Tel: +34 932 240 894, Fax: +34 932 240 875, E-mail: [email protected]
Received: 5 May 2003/  Accepted: 11 July 2003/

Rosalia Pascual, José I. Borrell, Jordi Teixidó*
Analysis of selection methodologies for combinatorial library design.
Grup d’Enginyeria Molecular, Institut Químic de Sarriá (IQS), Universitat Ramon Llull, Via Augusta 390, E-08017 Barcelona, Spain.
* Author to whom correspondence should be addressed;
Received: 12 June 2003/  Accepted: 119 July 2003/

Pablo Cironi^ξ¥, Mercedes Álvarez, ^ξ¥* Fernando Albericio ^ξ‡*
1H NMR Spectroscopy with Internal and External Standards for the Quantification of Libraries
ξ Barcelona Biomedical Research Institute, Barcelona Science Park, University of Barcelona, 08028-Barcelona, Spain
¥ Laboratory of Organic Chemistry, Faculty of Pharmacy, University of Barcelona, 08028 Barcelona (Spain).
‡ Department Organic Chemistry, University of Barcelona, 08028 Barcelona (Spain).
* Author to whom correspondence should be addressed; E-mail : [email protected]; [email protected]
Received: 2 July 2003/  Accepted: 14 July 2003/

Emili Besalú^*,1, Robert Ponec² and Jesus Vicente de Julián-Ortiz¹
Running head: Agents Against Mycobacterium tuberculosis.
Virtual Generation of Agents Against Mycobacterium tuberculosis. A QSAR study.
1 Institute of Computational Chemistry, Universitat de Girona, Facultat de Ciències, Avda. Montilivi s/n, 17071 Girona, Spain.
2 Institute of Chemical Process Fundamentals, Czech Academy of Sciences, Prague 6, Suchdol 2, 165 02 Czech Republic.
* Author to whom correspondence should be addressed; Tel: +34 972 418875, FAX: +34 972 418150, E-mail : [email protected]
Received: 29 April 2003/  Accepted: 15 July 2003/

Special issue on Proceedings of 2nd International Conference on Multi Component Reactions, Combinatorial and Related (Guest edited by Dr. Luca Banfi)

Rodolfo Lavilla^1,2* ,  Inés Carranco¹, José Luis Díaz¹, M. Carmen Bernabeu¹, and Guillermo de la Rosa¹
Dihydropyridines in MCRs. Tandem processes leading to modular tetrahydroquinoline systems with up to 6 diversity elements
1 Parc Científic de Barcelona, Josep Samitier, 1-5, 08028 Barcelona, Spain.
2 Laboratory of Organic Chemistry, Faculty of Pharmacy, University of Barcelona, Av. Joan XXIII, sn, 08028 Barcelona, Spain.
* Author to whom correspondence should be addressed; Fax:(+34)934037225; E-mail: [email protected]
Received: 9 April 2003/ Accepted: 26 April 2003/

Stefania Fioravanti,^* Alberto Morreale, Lucio Pellacani^*, and Paolo A. Tardella^*
Functionalised enones as starting materials for the construction of aziridine scaffolds
Dipartimento di Chimica, Università degli Studi di Roma “La Sapienza”, P.le Aldo Moro 2, I-00185 Roma, Italy
* Corresponding authors; Fax: +39-06-490631 E-mail: [email protected], [email protected]
Received: 9 April 2003/ Accepted: 8 May 2003/

Shin Kamijo,¹ Tienan Jin, Zhibao Huo, Young Soo Gyoung, Jae-Goo Shim, and Yoshinori Yamamoto²*
Tetrazole Synthesis via the Palladium-Catalyzed Three Component Coupling Reaction
1 Research Center for Sustainable Materials Engineering, Institute of Multidisciplinary Research for Advanced Materials;
2Department of Chemistry, Graduate School of Science, Tohoku University, Sendai 980-8578, Japan
* Author to whom correspondence should be addressed; E-mail: [email protected]
Received: 9 April 2003/ Accepted: 12 May 2003/

Maxim A. Mironov,* Maria N. Ivantsova, and Vladimir S. Mokrushin
Ugi reaction in aqueous solutions: a simple protocol for libraries production
Department of Technology of Organic Synthesis (TOSLab), Urals State Technical University, 620002 Ekaterinburg, Russian Federation
*Author to whom correspondence should be addressed; Fax +7 3432 754135; E-mail: [email protected]
Received: 19 April 2003/ Accepted: 13 May 2003/

Ahmad Shaabani,¹* Mohammad Bagher Teimouri,¹ Ayoob Bazgir¹, and Hamid Reza Bijanzadeh²
Introducing a novel class of four-component reactions
1 Department of Chemistry, Shahid Beheshti University, Zip Code 1983963113, Tehran, Iran
2 Department of Chemistry, Tarbiat Modarres University, P. O. Box 14155-4838, Tehran, Iran
Author to whom correspondence should be addressed; fax: +98-21-2403041 ; E-mail: [email protected]
Received: 19 February 2003/ Accepted: 19 May 2003/

Tatiana N. Borisova, Leonid G.Voskressensky* , Tatiana A. Soklakova, Larisa N. Kulikova & Alexey V. Varlamov
Cleavage of Some Annulated Tetrahydropyridines Under the Action of Dimethyl Acetylene Dicarboxylate in Protic Solvents. New practical route to substituted pyrroles and indoles
Organic Chemistry Department of the Russian Peoples Friendship University, 6, Miklukho-Maklaya St., Moscow, 117198 , Russia
* Author for correspondence ,Tel. 7-095-955-0849, Fax 7-095-954-0336, E-mail: [email protected]
Received: 20 March  2003/  Accepted: 27 May 2003/

Kuangsen Sung*, Fu-Lin Chen, and Meng-Jung Chung
Application of MCR: Facile one-pot diastereoselective syntheses of novel chiral a,a’- iminodiacetic acid analogues
Department of Chemistry, National Cheng Kung University, Tainan, Taiwan, ROC
*Author to whom correspondence should be addressed; E-mail: [email protected]
Received: 17 March 2003/ Accepted: 3 June 2003/

Javad Azizian*, Ali R. Karimi, Hamedeh Arefrad, Ali A. Mohammadi and M. R. Mohammadi zadeh
A novel one-pot, four component synthesis of some densely functionalized pyrroles
Department of Chemistry, Faculty of Science, Shahid Beheshti University, P. O. Box 19395-4716, Tehran, Iran. E-mail : [email protected]
Received: 4 May 2003/  Accepted: 5 June 2003/

Luca Banfi, Andrea Basso,* Giuseppe Guanti and Renata Riva
Passerini reaction – Amine Deprotection – Acyl Migration (PADAM): a convenient strategy for the solid-phase preparation of peptidomimetic compounds
Università degli Studi di Genova, Dipartimento di Chimica e Chimica Industriale, Via Dodecaneso 31, 16146 Genova, Italy
* Author for correspondence, Fax: +39 010 353 6118, E-mail: [email protected]
Received: 21 May 2003/  Accepted: 5 June 2003/

Claude V. Robotham¹, Christopher Baker,¹ Brian Cuevas,² Khalil Abboud^1§ and Dennis L. Wright¹*
A Multi-Component Reaction (MCR) Approach to the Synthesis of Highly Diverse Polymers with Polypeptide-Like Features
1 Department of Chemistry, University of Florida, Gainesville, FL, 32611, USA
2 Department of Material Science and Engineering, University of Florida, Gainesville, Fl, 32611, USA
§ Author to whom questions regarding x-ray crystal structures should be addressed.
* Author for correspondence, E-mail: [email protected]
Received: 7 May 2003/  Accepted: 11 June 2003/

Andrea Trabocchi, Francesco Mancini, Gloria Menchi & Antonio Guarna*
A Solid-Phase Approach Towards the Development of 3-Aza-6,8-Dioxabicyclo[3.2.1]Octane Scaffolds
Dipartimento di Chimica Organica "Ugo Schiff", Università degli Studi di Firenze, Polo Scientifico di Sesto Fiorentino, Via della Lastruccia 13, Sesto Fiorentino, I-50019 Firenze, Italy
* Author for correspondence, Tel. +39-055-457-3481, Fax +39-055-457-3569, E-mail: [email protected]
Received: 9 May 2003/  Accepted: 12 June 2003/

Roland U. Braun, and Thomas J. J. Müller*
Coupling-Isomerization-Coupling Sequences Switched On By Propargyl Alcohol-Enone-Isomerization
Organisch-Chemisches Institut der Ruprecht-Karls-Universität Heidelberg Im Neuenheimer Feld 270, D-69120 Heidelberg E-mail: [email protected]
Received: 30 May 2003/  Accepted: 13 June 2003/

Alessandro Dondoni* and Alessandro Massi
Decoration of Dihydropyrimidine and Dihydropyridine Scaffolds with Sugars via Biginelli and Hantzsch Multicomponent Reactions: an Efficient Entry to a Collection of Artificial Nucleosides
Dipartimento di Chimica, Università di Ferrara, Via L.Borsari, 46-44100 Ferrara, Italy.
* Author for correspondence,  Tel. +39 0532 291176; Fax +39 0532 291167 E-mail: [email protected]
Received: 30 May 2003/  Accepted: 18 June 2003/

Leon W. A. van Berkom, George J.T. Kuster and Hans W. Scheeren*
High pressure: a promising tool for multicomponent reactions
Department of Organic Chemistry, University of Nijmegen, Toernooiveld 1, 6525 ED Nijmegen, The Netherlands. E-mail: [email protected]
Received: 30 May 2003/  Accepted: 25 June 2003/

Sangwon Cho, Gyochang Keum, Soon Bang Kang, So-Yeop Han† and Youseung Kim*
An Efficient Synthesis of 2,5-Diketopiperazine Derivatives by the Ugi Four-Center Three-Component Reaction
Biochemicals Research Center, Korea Institute of Science and Technology, P.O.Box 131, Cheongryang, Seoul 130-650, Korea;
† Department of Chemistry and Division of Molecular Life Sciences, Ewha Womans University, Seoul, 120-750, Korea
* Author for correspondence, Tel: 82-2-958-5001 Fax: 82-2-958-5189, E-mail:[email protected]
Received: 20 May 2003/  Accepted: 1 July 2003/

Rajesh Kumar,^1,2 Rahul Tyagi,^2,3 Virinder S. Parmar,^1,3* Lynne A. Samuelson,⁴ Jayant Kumar² and Arthur C. Watterson^1*
Enzymatic Synthesis of Multi-component Copolymers and their Structural Characterization
1 Institute for Nano Science and Engineering Technology, Department of Chemistry, University of Massachusetts Lowell, MA 01854, USA
2 Center for Advanced Materials, Department of Chemistry and Physics, University of Massachusetts Lowell, MA 01854, USA
3 Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India
4 Natick Soldier Center, U.S. Army Soldier and Biological Chemical Command, Kansas Street, Natick, MA 01760, USA
* Author to whom correspondence should be addressed; Phone: +1-978-934-3691, Fax: +1-978-458-9571;E-mail: [email protected]
Received: 30 May 2003/  Accepted: 3 July 2003/

Jürgen Kolb, ² Barbara Beck,¹ Michael Almstetter,¹ Stefan Heck,¹ Eberhardt Herdtweck,³ Alexander Dömlinga,^2*
New MCRs: The First 4-Component Reaction Towards 2,4-Disubstituted Thiazoles
1 Morphochem AG, Gmunderstr.37-37a, 81379 München, Germany
2 Institut für Organische Chemie und Biochemie, Technische Universität München, Lichtenbergstr.4, 85747 Garching, Germany
3 Institut für Anorganische Chemie, Technische Universität München, Lichtenbergstr.4, 85747 Garching, Germany
* Author to whom correspondence should be addressed; Tel: ++4989780050; fax: ++498978005555; e-mail: [email protected]
Received: 30 May 2003/  Accepted: 10 July 2003/

Stanisław Ostrowski ^1,2,* and Agnieszka Mikus ¹
A New Approach to the Synthesis of Porphyrin–Fullerene Dyads#)
1 Institute of Chemistry, University of Podlasie, ul. 3 Maja 54, 08-110 Siedlce, Poland
2 Institute of Organic Chemistry, Polish Academy of Sciences, ul. Kasprzaka 44/52, 01-224 Warszawa, Poland
* Author to whom correspondence should be addressed; E-mail : [email protected]
Received: 30 May 2003/  Accepted: 25 July 2003/

Maria S. Zhidovinova , Olga V. Fedorova, Gennady L. Rusinov, Irina G. Ovchinnikova
Multicomponent sonochemical synthesis of podands
Institute of Organic Synthesis of RAS, 22, S.Kovalevskoy st., Yekaterinburg, GSP-147, 620219, Russia
* Author to whom correspondence should be addressed;  
Received: 10 July 2003/  Accepted: 5 September 2003/

Special issue on Structure/Function/SAR and Computational Chemistry/Molecular Design (Guest edited by Dr. György M. Keseru)

Jaroslaw Polanski, Rafal Gieleciak
The Comparative Molecular Surface Analysis: A Novel Tool for Drug Design and Molecular Diversity Studies
Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40-006 Katowice, Poland, e-mail: [email protected]
Received: 14 March 2003/  Accepted: 29 May 2003/

Gergely M. Makara,* Huw Nash, Zhongli Zheng, Jean-Paul A. Orminati and Edward A. Wintner
A Reagent-Based Strategy For the Design of Large Combinatorial Libraries: A Preliminary Experimental Validation
NeoGenesis Pharmaceuticals Inc., 840 Memorial Drive, Cambridge, Massachusetts, 02139
* Author to whom correspondence should be addressed. Phone: 617-588-5112, Fax: 617-868-1515, e-mail: [email protected]
Received: 24 March 2003/  Accepted: 10 June 2003/

Monique Laberge^a, Takashi Yonetani^b and Judit Fidy^a*
Normal Coordinate Structural Decomposition of the Heme Distortions of Hemoglobin in various quaternary states and bound to allosteric effectors
a Institute of Biophysics and Radiation Biology, Semmelweis University, Puskin u. 9, Budapest H-1088, Hungary. Phone: 36-1-267-6261; fax: 36-1-266-6656. E-mail: [email protected]; [email protected]
b Department of Biochemistry and Biophysics, Johnson Research Foundation, University of Pennsylvania, Philadelphia, PA 19104-6059. Phone: 215-898-8787; fax: 215-898-8559 E-mail: [email protected]
Received: 20 March 2003/  Accepted: 11 June 2003/

László Hackler Jr.¹, György Dormán², Zoltán Kele³, László Ürge², Ferenc Darvas^{2 4} and László G. Puskás¹*
Development of chemicaly modified glass surfaces for nucleic acid, protein and small molecule microarrays
1 Laboratory of Functional Genomics, Biological Research Center, H-6701, Szeged, Temesvári krt. 62
2 ComGenex Inc, H-1027 Budapest, Bem rkp 33-34
3 Department of Medicinal Chemistry, University of Szeged, Dóm tér 8, H-6720 Szeged, Hungary
4 ComGenex International, South San Francisco, California 94080, 705 Grandview Drive
Received: 20 March 2003/  Accepted: 13 June 2003/

László Molnár*¹, István Vágó², András Fehér³
Construction of a Linux based chemical and biological information system
1 Computer Assisted Drug Discovery, Gedeon Richter Ltd., P.O.Box 27, H-1475 Budapest, Hungary
2 Synthetic Lab II., Gedeon Richter Ltd., P.O.Box 27, H-1475 Budapest, Hungary
3 Chemical Information Technology, Technical University of Budapest, Szent Gellért tér 4., H-1111 Budapest, Hungary
* Corresponding author e-mail: [email protected]
Received: 20 March 2003/  Accepted: 13 June 2003/

Csaba Szántai-Kis^{1 5}, István Kövesdi^{2 3}, György Kéri1^{3 4}, László Őrfi1^{3 5*}
Validation subset selections for extrapolation oriented QSPAR models
1 Cooperative Research Center, Semmelweis University, Pf. 131, Budapest 5, Hungary, 1367, E-mail: [email protected]
2 EGIS Pharmaceuticals Ltd., Keresztúri u. 30-38, Budapest, Hungary, 1106
3 VICHEM Ltd., Hermann o. 15, Budapest, Hungary. 1022
4 Department of Medical Chemistry, Semmelweis University Peptide Biochemistry Research Group of the Hungarian Academy of Sciences, Puskin u. 9., Budapest, Hungary, 1088
5 Department of Pharmaceutical Chemistry, Semmelweis University, Hőgyes E. u. 9., Budapest, Hungary, 1092, Tel/Fax: +36-1-2170891, E-mail: [email protected]
* Corresponding author, E-mail: [email protected]
Received: 31 March 2003/  Accepted: 19 June 2003/

Special issue on Microwaves in Combinatorial and High-Throughput Synthesis (Guest edited by Dr. Oliver Kappe)

Gopal K. Datta, Karl S. A. Vallin, and Mats Larhed*
A Rapid Microwave Protocol for Heck Vinylation of Aryl Chlorides Under Air
Department of Organic Pharmaceutical Chemistry, Biomedical Centre, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden. Phone: +46 18 471 4667, Fax: +46 18 471 4474, E-mail: [email protected]
Received: 28 March 2003/  Accepted: 12 June 2003/

Angel Díaz-Ortiz*¹, Antonio de la Hoz¹, M. Antonia Herrero¹, Pilar Prieto¹, Ana Sánchez-Migallón¹, Fernando P. Cossio*², Ana Arrieta², Silvia Vivanco², Concepción Foces-Foces³
Enhancing Stereochemical Diversity by Means of Microwave Irradiation in the Absence of Solvent: Synthesis of Highly Substituted Nitroproline Esters via 1,3-Dipolar Reactions
1 Área de Química Orgánica, Facultad de Química, Universidad de Castilla-La Mancha, E-13071 Ciudad Real, Spain (E-mail: [email protected])
2 Departamento de Química Orgánica I, Facultad de Química, Universidad del País Vasco, Apto. 1072, 20080 Donostia – San Sebastian, Spain
3 Departamento de Cristalografía, Instituto de Química-Física ‘Rocasolano’, CSIC, Serrano 119, E-28006 Madrid, Spain
Received: 27 May 2003/  Accepted: 20 June 2003/

Hans Emtenäs, Camilla Taflin and Fredrik Almqvist*
Efficient Microwave Assisted Synthesis of Optically Active Bicyclic 2-Pyridinones via D2-Thiazolines
Organic Chemistry, Department of Chemistry, Umeå University, SE-901 87 Umeå, Sweden [email protected]
Received: 3 June 2003/  Accepted: 20 June 2003/

Kenneth A. Savin¹, Michael Robertson, Doug Gernert, Steven Green, Erik J. Hembre, Jessie Bishop
A Study of the Synthesis of Triazoles Using Microwave Irradiation
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285.
1 To whom correspondence should be addressed (e-mail: [email protected])
Received: 28 May 2003/  Accepted: 21 June 2003/

Wen-Ben Yeh, Mei-Jung Lin, Ming-Juan Lee and Chung-Ming Sun*
Microwave-Enhanced Liquid-Phase Synthesis of Thiohydantoins and Thioxotetrahydropyrimidinones
Laboratory of Combinatorial Drug Discovery, Department of Chemistry, National Dong Hwa University, Shou-Feng, Hualien-974, Taiwan
Corresponding author. Fax: +(886)-3-8630110; e-mail: [email protected]
Received: 7 June 2003/  Accepted: 23 June 2003/

Murugaiah M. S. Andappan, Peter Nilsson, Mats Larhed*
Arylboronic Acids as Versatile Coupling Partners in Fast Microwave Promoted Oxidative Heck Chemistry.
Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry, Biomedical Centre, Uppsala University, P. O. Box 574, SE-751 23, Uppsala, Sweden. Phone: +46 18 4714667, fax: +46 18 4714474, e-mail: [email protected]
Received: 27 May  2003/  Accepted: 23 June 2003/

Nadya Kaval,¹ Katalin Bisztray,¹ Wim Dehaen,¹ C. Oliver Kappe² & Erik Van der Eycken*¹
Microwave-enhanced transition metal-catalyzed decoration of 2(1H)-pyrazinone scaffolds
1 Laboratory for Organic Synthesis, Department of Chemistry, University of Leuven, Celestijnenlaan 200F, B-3001 Leuven;
2 Institute of Chemistry, Karl-Franzens-University Graz, Heinrichstrasse 28, A-8010 Graz, Austria
* Author for correspondence, Tel. +32 16327406, Fax: +32 16327990  E-mail: [email protected]
Received: 16 May 2003/  Accepted: 24 June 2003/

Núria Mont,^a Jordi Teixidó,^a C. Oliver Kappe ^b, and José I. Borrell^a*
A one-pot microwave-assisted synthesis of pyrido[2,3-d]pyrimidines
a Grup d'Enginyeria Molecular, Institut Químic de Sarrià, Universitat Ramon Llull, Via Augusta 390, E-08017 Barcelona, Spain;
b Institute of Chemistry, Karl-Franzens-University Graz, Heinrichstrasse 28,A-8010 Graz, Austria
* Address for correspondence, Grup d'Enginyeria Molecular Institut Quimic de Sarria Via Augusta 390 E-08017 Barcelona (Spain), tel: +34-932 672 000, fax: +34-932 056 266, e-mail: [email protected]
Received: 3 May 2003/  Accepted: 26 June 2003/

Fredrik Lehmann,¹ Åke Pilotti² and Kristina Luthman^1*
Efficient large scale microwave assisted Mannich reactions using substituted acetophenones
Running head: Microwave Assisted Mannich Reactions
1 Department of Chemistry – Medicinal Chemistry, Göteborg University, SE-412 96 Göteborg, Sweden;
2 Personal Chemistry, SE-753 18 Uppsala, Sweden and Department of Organic Chemistry, Stockholm University, SE-106 91 Stockholm, Sweden
* Department of Chemistry – Medicinal Chemistry, Göteborg University, SE-412 96 Göteborg, Sweden. Tel: +46-31-772 2894, Fax: +46-31-772 3840, E-mail: [email protected]
Received: 23 May 2003/  Accepted: 27 June 2003/

Nicholas E. Leadbeater^1,*, Hanna M. Torenius ¹ and Heather Tye²
Microwave-assisted Mannich-type three-component reactions
1 Department of Chemistry, King’s College London, Strand, London WC2R 2LS United Kingdom
2 Evotec OAI, 151 Milton Park, Abingdon, Oxfordshire, OX14 4SD United Kingdom
* Author to whom correspondence should be addressed; E-mail :  [email protected]
Received: 3 June 2003/  Accepted: 4 July 2003/

Klaus Weigand* and Sylvie Pelka
Microwave-assisted Pd(0)-catalyzed Amination of Aryl Halides on Solid Support
Novartis Research Institute, Medicinal Chemistry Unit, Brunner Strasse 59 A-1235 Vienna, Austria
* Author to whom correspondence should be addressed; Tel. ++43-1-86634-9050, Fax ++43-1-86634-354; E-mail :  [email protected]
Received: 19 June 2003/  Accepted: 4 July 2003/

Michael G. Organ,* Stanislas Mayer, Franck Lepifre, Blaise N'Zemba and Jayantilal Khatri
Combining The Use of Solid-Supported Transition Metal Catalysis With Microwave Irradiation In Solution-Phase Parallel Library Synthesis.
The Department of Chemistry York University, 4700 Keele Street, Toronto, Ontario, Canada, M3J 1P3
* Author to whom correspondence should be addressed; E-mail : [email protected]"
Received: 16 June 2003/  Accepted: 13 July 2003/

Wei Zhang,* Yimin Lu, Christine Hiu-Tung Chen
Combination of Microwave Reactions with Fluorous Separations in the Palladium-Catalyzed Synthesis of Aryl Sulfides
Fluorous Technologies, Inc. University of Pittsburgh Applied Research Center, 970 William Pitt Way, Pittsburgh, PA 15238, USA.
* Author to whom correspondence should be addressed; Tel: +1-412-826-3062, fax: +1-412-826-3053, E-mail: [email protected]
Received: 10 June 2003/  Accepted: 14 July 2003/

Stefano Crosignani, Delphine Launay, Bruno Linclau* and Mark Bradley*
Microwaves, supported-reagents and parallel synthesis: Isocyanide and ester synthesis
Combinatorial Centre of Excellence, Department of Chemistry, University of Southampton, Highfield, Southampton, SO17 1BJ, UK
Author to whom correspondence should be addressed; E-mail : [email protected]
Received: 28 May 2003/  Accepted: 22 July 2003/

François-René Alexandre, Lisianne Domon, Stéphane Frère, Alexandra Testard, Valérie Thiéry & Thierry Besson*
Microwaves in the Multi-Step Synthesis of Nitrogen/Sulfur Heterocycles
LGPC UPRES EA3169, Groupe de Chimie Organique UFR Sciences Fondamentales et Sciences pour l'Ingénieur,
Université de la Rochelle, Bâtiment Marie-Curie, F-17042 La Rochelle Cedex 1, France.
* Author to whom correspondence should be addressed; Tel: 33 5 46 45 82 76, Fax: 33 5 46 45 82 23, E-mail: [email protected]
Received: 3 June 2003/  Accepted: 22 July 2003/

Jaromír Literák,¹ Stanislav Relich,¹ Petr Kulhánek,² & Petr Klán ^1,*
Temperature dependent photochemical cleavage of 2,5-dimethylphenacyl esters
1 Department of Organic Chemistry, Faculty of Science, Masaryk University, Kotlarska 2, 611 37 Brno, Czech Republic. Fax: +420-541129641; Tel. +420-541129356; 
2 National Centre for Biomolecular Research, Faculty of Science, Masaryk University, Kotlarska 2, 611 37 Brno, Czech Republic.
* Author to whom correspondence should be addressed; E-mail : [email protected]
Received: 20 June 2003/  Accepted: 25 July 2003/

Doris Dallinger, Nikolay Yu. Gorobets and C. Oliver Kappe*
Microwave-Assisted Scavenging of Electrophiles Utilizing Polymer-Supported Sequestration Reagents. Application to the Synthesis of N3-Acylated Dihydropyrimidine Libraries
Institute of Chemistry, Karl-Franzens-University Graz, Heinrichstrasse 28, A-8010 Graz, Austria
* Author to whom correspondence should be addressed; Tel: +43-316-3805352; Fax: +43-316-3809840 E-mail: [email protected]
Received: 17 June 2003/  Accepted: 31 July 2003/

Jon-Sverre Schanche
Microwave Synthesis Solutions from Personal Chemistry
Personal Chemistry AB, Kungsgatan 76, SE-753 18 Uppsala, Sweden.
* Author to whom correspondence should be addressed; Tel. +46 18 489 9019, Fax: +46 18 489 9100, Email: [email protected]
Received: 4 June 2003/  Accepted: 1 August 2003/

Laura Favretto*
Milestone's Microwave Labstation
Milestone srl, Via Fatebenefratelli 1/5, 24010 Sorisole (BG), Italy
* Author to whom correspondence should be addressed; Tel.++39 035.573857, Fax ++39 035.575498, E-mail: [email protected]
Received: 3 June 2003/  Accepted: 28 August 2003/

Robb Nicewonger*, April Fowke, Kathy Nguyen, Lori Ditto, Justin Caserta, Michele Harris, and Carmen M. Baldino
Microwave-Assisted Acylation of 7-Amino-5-aryl-6-cyanopyrido[2,3-d]pyrimidines
ArQule, Inc. 19 Presidential Way, Woburn, MA 01801 USA.
* Author to whom correspondence should be addressed; Tel: (781) 994-0496, E-mail: [email protected]
Received: 8 August 2003/  Accepted: 29 August 2003/

Matthias Nüchter, Bernd Ondruschka
Tools for Microwave-Assisted Parallel Syntheses and Combinatorial Chemistry
Institute of Technical Chemistry and Environmental Chemistry, Friedrich Schiller University Jena, Lessingstr. 12, D-07743 Jena, Germany.
* Author to whom correspondence should be addressed; Phone: +49 3641 948413, Fax: +49 3641 948402, E-mail: [email protected]
Received: 10 June 2003/  Accepted: 9 September 2003/

Thomas E. Vasquez Jr., Thomas Nixey, Balan Chenera, Vijay Gore, Mike Bartberger^#, Yax Sun^#, and Christopher Hulme^*
One-Pot Microwave Assisted Preparation of Pyrazoloquinazolinone Libraries
#Molecular Structure, Chemistry Research and Development, AMGEN, One AMGEN Center Drive, Thousand Oaks, CA 91320.
* Author to whom correspondence should be addressed; Medicinal Chemistry Technologies, Chemistry Research and Development, AMGEN, One AMGEN Center Drive, Thousand Oaks, CA 91320. [email protected]
Received: 4 September 2003/  Accepted: 10 September 2003/

Published Papers

Juntao Luo and Wenqiang Huang*
A New Strategy for Solid Phase Synthesis of a Secondary Amide Library Using Sulfonamide Linker via Radical Traceless Cleavage 
State Key Laboratory of Polymer Materials for Adsorption and Separation, Institute of Polymer Chemistry, Nankai University, Tianjin 300071, P. R. China Tel: +86-22-23501411 Ext. 805 Fax: +86-22-23503510
*To whom correspondence should be addressed:
E-mail address: [email protected]
Received: 26 September 2002/  Accepted: 10 November 2002/

Claudia Riva-Toniol ¹, Sascha Müller, Josette Schaub ² and Wolfgang K.-D. Brill ³*
2, 6, 8-Trisubstituted Purines Catalysis of Nucleophilic Aromatic Substitutions in the 2, 6, 8-Trisubstituted Purines and Application in the Synthesis of Combinatorial Libraries
1 Pharmazentrum der Universitaet Basel, Klingenbergstr. 50 – 70, CH-4056 Basel, Switzerland
2 Novartis Pharma AG, Lichtstrasse 35, CH-4056 Basel, Switzerland
3* Present address: Pharmacia Italia S.p.A, Viale Pasteur, 10, 20014 Nerviano (Mi), Italy.Tel: +39 02 4838 5144, FAX: +39 02 4838 3833
E-mail: [email protected]
Received: 11 February 2003/  Accepted: 24 April 2003/

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