PROCESS FOR PRODUCING (R)-2-HYDROXY-1-PHENOXYPROPANE DERIVATIVE
    43.
    发明公开
    PROCESS FOR PRODUCING (R)-2-HYDROXY-1-PHENOXYPROPANE DERIVATIVE 审中-公开
    生产(R)-2-羟基-1-苯氧基丙烷衍生物的方法

    公开(公告)号:EP1055732A1

    公开(公告)日:2000-11-29

    申请号:EP99959901.2

    申请日:1999-12-20

    IPC分类号: C12P7/22

    CPC分类号: C12P7/22 C12P41/002

    摘要: The present invention is related to producing (R)-2-hydroxy-1-phenoxypropane derivatives, which are of value as intermediates of pharmaceuticals, with high optical purity and good efficiency,

    comprising a step of reducing a phenoxyacetone derivative with a carbonyl reductase derived from a microorganism of the genus Candida or a culture broth or processed culture broth of said microorganism having the ability to elaborate the carbonyl reductase.

    摘要翻译: 本发明涉及生产具有高光学纯度和高效率的作为药物中间体的(R)-2-羟基-1-苯氧基丙烷衍生物,该方法包括用衍生的羰基还原酶还原苯氧基丙酮衍生物的步骤 来自假丝酵母属的微生物或培养肉汤或所述微生物的加工过的培养肉汤,其能够精制所述羰基还原酶。

    PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE 2- 6-(HYDROXYMETHYL)-1,3-DIOXAN-4-YL]ACETIC ACID DERIVATIVES
    44.
    发明公开
    PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE 2- 6-(HYDROXYMETHYL)-1,3-DIOXAN-4-YL]ACETIC ACID DERIVATIVES 有权
    VERFAHREN ZUR HERSTELLUNG OPTISCH AKTIVER 2-(6-(羟甲基)-1,3-DIOXAN-4-YL)-ESSIGSÄURE-DERIVATE

    公开(公告)号:EP1024139A1

    公开(公告)日:2000-08-02

    申请号:EP99935066.3

    申请日:1999-08-05

    摘要: This invention provides a process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl] acetic acid derivatives, which are of value as intermediates of drugs, from inexpensive starting materials without using any special equipment such as that required for super-low temperature reactions.
    A process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives which comprises

    reacting an acetic acid derivative at a temperature of not less than -30°C with an enolate prepared by permitting either a base or a metal having a valency of 0 to act on the derivative to produce a hydroxyoxohexanoic acid derivative,
    reducing this compound with the aid of a strain of microorganism to provide a halomethyldioxanylacetic acid derivative,
    treating this compound with an acetalizing agent in the presence of an acid catalyst to provide a halomethyldioxanylacetic acid derivative,
    reacted with an acyloxylating agent to provide a acyloxymethyldioxanylacetic acid derivative, and
    subjecting this compound to solvolysis in the presence of a base.

    摘要翻译: 本发明提供了一种从廉价起始原料生产具有价值作为药物中间体的光学活性2-δ-(羟甲基)-1,3-二恶烷-4-基乙酸衍生物的方法,而不使用任何特殊设备,例如 这是超低温反应所需的。 一种制备光学活性的2-δ-(羟甲基)-1,3-二恶烷-4-基乙酸衍生物的方法,其包括使不饱和-30℃的乙酸衍生物与通过使任一种 碱或金属,其化合价为0,作用于衍生物以产生羟基己酸衍生物,借助微生物菌株还原该化合物,得到卤代甲基二恶烷基乙酸衍生物,在缩合剂存在下用缩醛化剂处理该化合物 的酸催化剂,得到卤代甲基二恶烷基乙酸衍生物,与酰氧基化剂反应,得到酰氧基甲基二恶烷基乙酸衍生物,并在碱的存在下使其溶解。