A Practical Synthesis of a Diazepinylbenzoic Acid, a Retinoid X Receptor Antagonist
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  • 作者：Xinglong Jiang ; George T. Lee ; Kapa Prasad ; Oljan Repi
  • 刊名：Organic Process Research & Development
  • 出版年：2008
  • 出版时间：November 21, 2008
  • 年：2008
  • 卷：12
  • 期：6
  • 页码：1137-1141
  • 全文大小：177K
  • 年卷期：v.12,no.6(November 21, 2008)
  • ISSN：1520-586X
文摘
An optimized convergent synthetic route for the preparation of retinoid X receptor (RXR) antagonist (1) in an overall yield of 35% is described. The formation of the benzodiazepine was achieved in 85% yield using POCl3 in toluene. The drug substance 14 was obtained by treatment of aryl bromide with vinyl butyl ether in the presence of palladium acetate, DPPP, and cesium carbonate This one-pot operation incorporating three chemical transformations (i.e., Heck reaction, hydrolysis of vinyl ether, and hydrolysis of ester) was achieved in 85% yield.
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