Multicomponent Synthesis of Diverse 1,4-Benzodiazepine Scaffolds

被引：55

作者：

Huang, Yijun ^{[1
]}

Khoury, Kareem ^{[1
,2
]}

Chanas, Tyler ^{[1
]}

Domling, Alexander ^{[1
,2
]}

机构：

[1] Univ Pittsburgh, Sch Pharm, Dept Pharmaceut Sci, Pittsburgh, PA 15261 USA

[2] Univ Groningen, Dept Drug Design, NL-9713 AV Groningen, Netherlands

来源：

ORGANIC LETTERS | 2012年 / 14卷 / 23期

关键词：

SOLUTION-PHASE PREPARATION; ONE-POT SYNTHESIS; DISCOVERY; CHEMISTRY; QUINOLIN-2-(1H)-ONES; GENERATION; LIBRARY; ANALOGS; DESIGN;

D O I：

10.1021/ol302837h

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The 1,4-benzodiazepine (BDZ) scaffold is of particular interest in drug design due to a balanced ensemble of beneficial physicochemical properties including a semirigid and compact diazepine ring with spatial placements of several substituents, combined with low number of rotatable bonds, hydrogen bond donors and acceptors, and intermediate lipophilicity. As an alternative to traditional multistep sequential syntheses, we designed routes employing one-pot MCRs to accelerate access diverse BDZ scaffolds in two or three steps.

引用

页码：5916 / 5919

页数：4

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