发明名称 PROCESS FOR THE PRODUCTION OF ESTETROL INTERMEDIATES
摘要 The present invention relates to a process for the preparation of a compound of formula (I)comprising the steps of a) reacting a compound of formula (II) with a silylating or an acylating agent to produce compound of formula (III), wherein Pis a protecting group selected from R-Si-RRor RCO-, wherein Ris a group selected from Calkyl or Ccycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or Calkyl; R, Rand Rare each independently a group selected from Calkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or Calkyl:b) halogenation or sulfinylation of the compound of formula (III) to produce a compound of formula (IV); wherein X is halo, or -O-SO-R, and Ris a group selected from Caryl or heteroaryl, each group being optionally substituted by one or more substituents independently selected from chloro or Calkyl:c) dehalogenation or desulfinylation of the compound of formula (IV) to produce a compound of formula (V)d) reacting the compound of formula (V) with a reducing agent to produce the compound of formula (I).
申请公布号 EA025511(B1) 申请公布日期 2016.12.30
申请号 EA20130001315 申请日期 2012.06.01
申请人 ESTETRA S.P.R.L. 发明人 PASCAL Jean-Claude
分类号 C07J75/00;A61K31/565;A61P15/12 主分类号 C07J75/00
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