One-Pot Homologation of Boronic Acids: A Platform for Diversity-Oriented Synthesis
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- 作者：Calum W. Muir ; Julien C. Vantourout ; Albert Isidro-Llobet ; Simon J. F. Macdonald ; Allan J. B. Watson
- 刊名：Organic Letters
- 出版年：2015
- 出版时间：December 18, 2015
- 年：2015
- 卷：17
- 期：24
- 页码：6030-6033
- 全文大小：367K
- ISSN：1523-7052
文摘
Formal homologation of sp2-hybridized boronic acids is achieved via cross-coupling of boronic acids with conjunctive haloaryl BMIDA components in the presence of a suitably balanced basic phase. The utility of this approach to provide a platform for diversity-oriented synthesis in discovery medicinal chemistry is demonstrated in the context of the synthesis of a series of analogues of a BET bromodomain inhibitor.