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6-烷基氨基-2-(官能化氨甲基)-2H-1-苯并吡喃文库的固相平行合成方法

Method for the solid-phase parallel synthesis of a 6-alkylamino-2-(functionalized-aminomethyl)-2H-1-benzopyran Library.

作者信息

Hwang Jong Yeon, Choi Hyung-Sub, Seo Jin-soo, La Hyun-Ju, Yoo Sung-eun, Gong Young-Dae

机构信息

Medicinal Science Division, Korea Research Institute of Chemical Technology, Yusung-gu, Daejeon 305-600, Korea.

出版信息

J Comb Chem. 2006 Nov-Dec;8(6):897-906. doi: 10.1021/cc0600526.

DOI:10.1021/cc0600526
PMID:17096579
Abstract

A 2000-member library of benzopyran analogues was prepared by using a solid-phase synthesis protocol. Polymer-bound 6-alkylaminobenzopyrans 7 were synthesized as part of a first generation diversification step by employing reactions of a variety of alkyl halides with the amine 6. Transformations of the resin-bound intermediates 8 formed in this manner by reactions with acid halides, sulfonyl chlorides, and isocyanates leads to introduction of the second level of diversification found in the series of 6-alkylamino-2-(functionalized-aminomethyl)-2-methyl-2H-1-benzopyran analogues 11 and 12.

摘要

通过使用固相合成方案制备了一个包含2000个成员的苯并吡喃类似物文库。作为第一代多样化步骤的一部分，通过使各种卤代烷与胺6反应，合成了聚合物负载的6-烷基氨基苯并吡喃7。通过与酰卤、磺酰氯和异氰酸酯反应以这种方式形成的树脂负载中间体8的转化，导致在6-烷基氨基-2-（官能化氨基甲基）-2-甲基-2H-1-苯并吡喃类似物系列11和12中引入了第二级多样化。

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