Preparation of chiral hydroxyketones
    3.
    发明公开
    Preparation of chiral hydroxyketones 失效
    Herstellung von chiralen Hydroxyketonen。

    公开(公告)号:EP0506341A1

    公开(公告)日:1992-09-30

    申请号:EP92302534.0

    申请日:1992-03-25

    发明人: Gala, Dinesh

    摘要: A process for preparing an hydroxyketone of the formula (X):

    wherein Ar represents substituted phenyl, aromatic heterocyclic, or substituted aromatic heterocyclic; R 1 and R 2 independently represents hydrogen, C-1 to C-16 alkyl, aromatic, substituted aromatic, aromatic heterocyclic, substituted aromatic heterocyclic or C-1 to C-5 alkyl covalently bonded to Ar, with the provision that R 1 and R 2 are different. The process comprises contacting a compound of the formula (V):

    with a solvent, a base and a chiral hydroxylating agent at a temperature of about -85°C or less.
    Compounds of the formulae


    also are disclosed.

    摘要翻译: 制备式(X)的羟基酮的方法:其中Ar表示取代的苯基,芳族杂环或取代的芳族杂环; R 1和R 2独立地表示氢,C 1至C 16烷基,芳族,取代的芳族,芳族杂环,取代的芳族杂环或与Ar共价结合的C-1至C-5烷基, R 1和R 2不同。 该方法包括在约-85℃或更低的温度下使式(V)化合物:与溶剂,碱和手性羟基化试剂接触。 也公开了式的化合物。

    Synthesis of azetidinones
    7.
    发明公开
    Synthesis of azetidinones 失效
    Synthese von Azetidinonen。

    公开(公告)号:EP0255278A1

    公开(公告)日:1988-02-03

    申请号:EP87306402.6

    申请日:1987-07-20

    摘要: A process for producing a compound having the formula
    wherein Pr is hydrogen or a hydroxy protecting group and Pr¹ is a carboxy protecting group, comprising reacting a compound of the formula
    wherein Pr is as previously defined, with a compound having the formula Pr¹-OH, wherein Pr¹ is as previously defined and either mineral acid or a silver salt of an organic base, and reacting the product so produced with a compound having the formula:
    wherein L is a leaving group.
    Three reaction schemes are disclosed as well as novel intermediate compounds.

    摘要翻译: 一种制备具有式CHEM的化合物的方法,其中Pr是氢或羟基保护基,Pr 1是羧基保护基,其包括使式(CHEM)化合物(其中Pr如前所定义)与 具有式Pr 1 -OH的化合物,其中Pr 1如前所定义,无机酸或有机碱的银盐,并使所得产物与具有下式的化合物反应: 其中L是离去基团。 公开了三种反应方案以及新的中间体化合物。