首页> 外国专利> A process for the preparation of precursor of Allyl sulfoxides inhibitors of Oak trees.

A process for the preparation of precursor of Allyl sulfoxides inhibitors of Oak trees.

机译:一种橡树烯丙基亚砜抑制剂前体的制备方法。

摘要

Method for preparing precursor of alilsulfoxidos Enzyme inhibitors of Structural formula (i), wherein R is phenyl, phenyl substituted with an electron withdrawing Group, or an Aromatic heterocycle trihalometilo five or six members; R is Hydrogen or aminometilo increased to 1; R Square R High and 5 are Hydrogen; R Cube is a group easily outgoingOr R R Square and Cube together form a double Bond; R is Hydrogen or a high 4 electron acceptor Group; R is Hydrogen or High 6 - COOH, and R is raised to 7 - Oh, - NH2, - SH and CH2OH.A man is to oxidize Aromatic Derivative of Structural formula (ii) wherein R and R increased to 1 - 7 have the meaning indicated above, with the exception of any of the substituents R high to 1 - 7 is sensitive to oxidation is provided with a protecting Group. After oxidation the Protecting Group is removed.The oxidizing Agent is selected from 1 - clorobenzotriazol, Cl2, Br2, naio4, ch3coono2o a peracido. * * n formula
机译:制备结构式(i)的烯丙硫氧化物的酶抑制剂的前体的方法,其中R为苯基,被吸电子基团取代的苯基或五或六元芳族杂环三卤代基; R是氢或氨基metilo增加到1; R Square R High和5为氢; R Cube是一个容易离去的基团,或者R R Square和Cube一起形成双键; R是氢或高4电子受体基团; R为氢或高6-COOH,并且R升高至7-OH,-NH2,-SH和CH2OH。一个人是要氧化结构式(ii)的芳香族衍生物,其中R和R增加到1-7时具有如上所指示的含义,除高至1至7的对氧化敏感的任何取代基R之外,其具有保护基。氧化后,除去保护基。氧化剂选自1-氯苯并三唑,Cl 2,Br 2,naio 4,ch 3 coono 2 o过酸。 * * n公式

著录项

  • 公开/公告号ES8106282A1

    专利类型

  • 公开/公告日1981-10-16

    原文格式PDF

  • 申请/专利权人 MERCK & CO.INC.;

    申请/专利号ES19800494302

  • 发明设计人

    申请日1980-08-14

  • 分类号C07C147/14;A61K37/64;

  • 国家 ES

  • 入库时间 2022-08-22 15:48:01

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