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Combinatorial Chemistry & High Throughput Screening

Editor-in-Chief

ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

Recent Developments in the Combinatorial Synthesis of Nitrogen Heterocycles Using Solid Phase Technology

Author(s): P.M.S. Chauhan and Sanjay K. Srivastava

Volume 4, Issue 1, 2001

Page: [35 - 51] Pages: 17

DOI: 10.2174/1386207013331327

Price: $65

Abstract

Recognizing the potential of combinatorial chemistry to accelerate drug discovery and development, most pharmaceutical and related industries are seriously looking towardcombinatorial synthesis of compounds in order to facilitate the identification of ‘lead’ molecules. In particular, solid phase synthesis is the core technology for combinatorial chemistry and is widely used for generating libraries of structurally related compounds. Since many drugs contain the nitrogen heterocylic component and since heterocycles posses a high order of structural diversity, a precise overview of recent progress in the combinatorial synthesis of nitrogen heterocycles using solid phase methodology would be useful. Since the progress in solid phase synthesis of organic molecules has been reviewed regularly from 1992 to 1998, only the development of solid phase combinatorial synthetic approaches of small nitrogen heterocylces since 1999 will be reviewed here. This review describes the solid phase synthesis of azepanes, benzodiazepines, benzimidazoles, benzothiazepines, cinnolines, indolizines, beta lactams, oxazepins, oxazoles including benzisooxazoles, hydantoins, piperidines, pyrimidines, pyrazolones, quinolones, trizolopyridazines and thiazoles.

Keywords: Combinatorial Synthesis, Nitrogen hetrocycle, azepanes, diisopropylcarbodiimide, amino resin, cinnamides, cinnolines, polymer bound


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