首页> 外国专利> Process for the preparation of 4-phosphinyl-3-keto-carboxylate and 4- phosphonyl-3-keto-carboxylate intermediates useful in the preparation of phosphorus containing HMG-CoA reductase inhibitors

Process for the preparation of 4-phosphinyl-3-keto-carboxylate and 4- phosphonyl-3-keto-carboxylate intermediates useful in the preparation of phosphorus containing HMG-CoA reductase inhibitors

机译:制备用于制备含磷的HMG-CoA还原酶抑制剂的4-膦酰基-3-酮-羧酸酯和4-膦酰基-3-酮-羧酸酯中间体的方法

摘要

A process for the preparation of compounds of formula ##STR1## or salt thereof where R.sub.1 is --X--Z and X is --C.tbd.C--,P PR. sub.2 and R.sub.2 ' are independently hydrogen, alkyl or trialkylsilyl; PPR.sub.3 is hydrogen or alkyl; and PPZ is a hydrophobic anchor;PPwhich includes reacting a compound of formula ##STR2## where R.sub.4 is alkyl, cycloalkyl or aryl; and R.sub. 5 is trialkylsilyl or triarylsilyl with a compound of formula ##STR3## where Y is a halogen, to form a compound of formula ##STR4## and hydrolyzing the compound of formula IV to obtain the compounds of formula I. Compounds of formula I or salt thereof where R. sub.1 is --OR.sub.2 ' may be prepared by reacting a compound of formula III with a compound of formulaPPP(OR.sub.2).sub.3 XII.
机译:制备式## STR1 ##化合物或其盐的方法,其中R1是-X-Z,X是-CtbdC-,

R 。 sub.2和Rsub.2'独立地是氢,烷基或三烷基甲硅烷基;

R.sub.3是氢或烷基; [0020] P

Z是疏水性锚;

其包括使式## STR2 ##的化合物反应,其中R4是烷基,环烷基或芳基;和R.sub。 5为三烷基甲硅烷基或三芳基甲硅烷基,具有式## STR3 ##的化合物,其中Y为卤素,形成式## STR4 ##的化合物并水解式IV的化合物以获得式I的化合物。 R.sub.1是-OR.sub.2'的I或其盐可以通过使式III的化合物与式P

P(OR.sub.2)的化合物反应来制备.3 XII。

著录项

  • 公开/公告号US5298625A

    专利类型

  • 公开/公告日1994-03-29

    原文格式PDF

  • 申请/专利权人 E. R. SQUIBB & SONS INC.;

    申请/专利号US19920987514

  • 发明设计人 WEN S. LI;JOHN K. THOTTATHIL;

    申请日1992-12-07

  • 分类号C07F7/02;C07F9/02;

  • 国家 US

  • 入库时间 2022-08-22 04:32:02

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