发明名称 PROCESS FOR THE PRODUCTION OF ESTETROL
摘要 The present invention relates to a process for the preparation of a compound of formula (I), hydrates or solvates thereof:said process comprising the steps of: a) reacting a compound of formula (II) with an acylating or a silylating agent to produce a compound of formula (III)wherein Pis a protecting group selected from RCO- or RSi(R)(R)-, Pis a protecting group selected from (RRR)C-CO- or (R)Si(R)(R)-, 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; Ris a group selected from Calkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or Calkyl; Rand Rare each independently hydrogen or a group selected from Calkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or Calkyl; b) reacting the compound of formula (III) in the presence of at least one oxidizing agent selected from permanganate salt, osmium oxide, hydrogen peroxide or iodine and silver acetate to produce a compound of formula (IV)and c) deprotecting the compound of formula (IV) to produce the compound of formula (I).
申请公布号 EA024003(B1) 申请公布日期 2016.08.31
申请号 EA20140090713 申请日期 2012.10.05
申请人 ESTETRA S.P.R.L. 发明人 PASCAL JEAN-CLAUDE
分类号 C07J75/00 主分类号 C07J75/00
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