Solid-Phase Parallel Synthesis of Drug-Like Artificial 2H-Benzopyran Libraries 英文参考文献.docVIP

Molecules 2012, 17, 5467-5496; doi:10.3390/moleculeOPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Review Solid-Phase Parallel Synthesis of Drug-Like Artificial 2H-Benzopyran Libraries Taeho Lee 1 and Young-Dae Gong 2,* 1 Research Institute of Pharmaceutical Sciences, College of Pharmacy, Kyungpook National University, 1370, Sangyuk-dong, Buk-gu, Daegu 702-701, Korea; E-Mail: tlee@knu.ac.kr 2 Center for Innovative Drug Library Research, Department of Chemistry, College of Natural Science, Dongguk University-Seoul, 26 Pildong 3-ga, Jung-gu, Seoul 100-715, Korea * Author to whom correspondence should be addressed; E-Mail: ydgong@; Tel.: +82-2-2260-3206; Fax: +82-2-2268-8204. Received: 10 April 2012; in revised form: 25 April 2012 / Accepted: 7 May 2012 / Published: 9 May 2012 Abstract: This review covers the construction of drug-like 2H-benzopyrans and related libraries using solid-phase parallel synthesis. In this context, the preparation of substituted benzopyrans such as mono-, di- and trisubstituted benzopyran derivatives and additional ring-fused benzopyrans such as benzopyranoisoxazoles, benzopyranopyrazoles, six-membered ring-fused benzopyrans, and polycyclic benzopyrans are highlighted. Keywords: combinatorial chemistry; solid-phase synthesis; chemical library; drug-like molecules; 2H-benzopyran 1. Introduction Combinatorial chemistry has become an extremely powerful technique for the generation of drug- like and biologically active small organic molecule libraries in either the solution-phase or on solid supports [1–5]. In combinatorial synthesis, solid-phase organic synthesis (SPOS) is now routinely used to prepare a large number of small heterocyclic molecules and is especially useful in creating massive numbers of hit and lead compounds as part of high-throughput screening (HTS) technologies [6–10]. This is especially true for the privileged structures, which are core components of a large n