Industrial Synthesis of 4-Chloro,11-arylestradiol: How to Circumvent a Poor Diastereoselectivity
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- 作者：Denis Prat ; Franç ; oise Benedetti ; Gilles Franc Girard ; Lahlou Nait Bouda ; John Larkin ; Christian Wehrey ; and Jacques Lenay
- 刊名：Organic Process Research & Development
- 出版年：2004
- 出版时间：March 2004
- 年：2004
- 卷：8
- 期：2
- 页码：219 - 228
- 全文大小：182K
- 年卷期：v.8,no.2(March 2004)
- ISSN：1520-586X
文摘
An industrial synthesis of 11
-arylestrone derivatives is described, based on the conjugate opening of a mixture of allylic5(10)-
and - epoxides by an aryl cuprate generated catalytically, followed by hydrolysis and subsequent aromatisation ofthe isomeric mixture of arylation products. An original methodfor selective 4-chlorination of estrone derivatives is also described.
-arylestrone derivatives is described, based on the conjugate opening of a mixture of allylic5(10)- and - epoxides by an aryl cuprate generated catalytically, followed by hydrolysis and subsequent aromatisation ofthe isomeric mixture of arylation products. An original methodfor selective 4-chlorination of estrone derivatives is also described.