Multicomponent synthesis of diverse 1,4-benzodiazepine scaffolds.
Multicomponent synthesis of diverse 1,4-benzodiazepine scaffolds.
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DOI：
10.1021/ol302837h
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发表时间：
2012-12-07
期刊：
影响因子：
5.2
通讯作者：
Domling, Alexander
中科院分区：
文献类型：
--
作者：
Huang, Yijun;Khoury, Kareem;Chanas, Tyler;Domling, Alexander
The 1,4-benzodiazepine (BDZ) scaffold is of particular interest in drug design due to a balanced ensemble of beneficial physicochemical properties including a semi-rigid 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.
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