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    PROCESS FOR PRODUCING SIMVASTATIN
    5.
    发明公开
    PROCESS FOR PRODUCING SIMVASTATIN 有权
    VERFAHREN ZUR HERSTELLUNG EINES SIMVASTATIN PRECURSORS

    公开(公告)号：EP1055671A1

    公开(公告)日：2000-11-29

    申请号：EP99959738.8

    申请日：1999-12-10

    申请人： KANEKA CORPORATION

    发明人： TAOKA, Naoaki ,  INOUE, Kenji

    IPC分类号： C07D309/30 ,  C07D319/06

    CPC分类号： C07D319/06 ,  C07D309/30 ,  Y02P20/55

    摘要： This invention provides an easy and efficient process for producing a simvastatin of great use as an HMG-CoA reductase inhibitor,

    which comprises deacylation of lovastatin with an inorganic base and a secondary or tertiary alcohol and subjecting the resulting did lactone to selective protection with a ketal or acetal protective group, acylation and deprotection-lactonization to give simvastatin.

    摘要翻译： 本发明提供了一种用于生产作为HMG-CoA还原酶抑制剂的伟大用途的辛伐他汀的简单和有效的方法，其包括用无机碱和仲或叔醇脱氢洛伐他汀，并使所得内酯用缩酮进行选择性保护 或缩醛保护基，酰化和去保护 - 内酯化得到辛伐他汀。

    PROCESS FOR PRODUCING OPTICALLY ACTIVE 3,5-DIHYDROXYCARBOXYLIC ACID DERIVATIVE
    6.
    发明授权
    PROCESS FOR PRODUCING OPTICALLY ACTIVE 3,5-DIHYDROXYCARBOXYLIC ACID DERIVATIVE 有权
    生产光学活性3,5-二羟基羧酸衍生物的方法

    公开(公告)号：EP1439162B1

    公开(公告)日：2008-03-26

    申请号：EP02777941.2

    申请日：2002-10-24

    申请人： KANEKA CORPORATION

    发明人： SUGAWARA, Masanobu ,  INOUE, Kenji

    IPC分类号： C07C69/675 ,  C07C69/78 ,  C07C67/31

    CPC分类号： C07C67/31 ,  C07B2200/07 ,  C07C67/29 ,  C07C69/78 ,  C07C69/675

    摘要： A process for producing an optically active 3,5-dihydroxyhexanoic acid derivative by stereoselectively reducing an optically active 3-oxo-5-hydroxyhexanoic acid derivative. It necessitates neither an ultralow-temperature reactor nor an incubator and is a simple and economical process in which protection of the 5-position hydroxy is unnecessary. Hydrogen, which is extremely inexpensive, is used as a reducing agent to asymmetrically hydrogenate an optically active 3-oxo-5-hydroxyhexanoic acid derivative by the catalytic action of a ruthenium/optically active phosphine complex, especially an RuBr2BINAP complex prepared from 2,2'-bisdiarylphosphino-1,1'-binaphthyl (BINAP) and a ruthenium complex, to thereby produce an optically active 3,5-dihydroxyhexanoic acid derivative.

    摘要翻译： 通过立体选择性还原光学活性的3-氧代-5-羟基己酸衍生物来制备光学活性3,5-二羟基己酸衍生物的方法。 它既不需要超低温反应器也不需要培养箱，并且是不需要保护5位羟基的简单且经济的过程。 使用非常便宜的氢作为还原剂，通过钌/旋光活性膦配合物的催化作用，使光学活性的3-氧代-5-羟基己酸衍生物不对称地氢化，特别是由2,2-二甲基-1,3-二氧戊环制备的RuBr2BINAP配合物 双 - 二芳基膦基-1,1'-联萘（BINAP）和钌配合物，由此制备光学活性的3,5-二羟基己酸衍生物。

    PROCESS FOR PREPARING OPTICALLY ACTIVE 2- 6-(HYDROXY-METHYL)-1,3-DIOXAN-4-YL|ACETIC ACID DERIVATIVES
    7.
    发明授权
    PROCESS FOR PREPARING OPTICALLY ACTIVE 2- 6-(HYDROXY-METHYL)-1,3-DIOXAN-4-YL|ACETIC ACID DERIVATIVES 有权
    用于生产光学活性的2-¬6-（羟甲基）-1,3-二恶烷-4-基| ACETIC衍生物（〇一年十二月十九日）

    公开(公告)号：EP1288213B1

    公开(公告)日：2006-11-29

    申请号：EP01936850.5

    申请日：2001-06-05

    申请人： KANEKA CORPORATION

    发明人： NISHIYAMA, Akira ,  HORIKAWA, Miho ,  YASOHARA, Yoshihiko ,  UEYAMA, Noboru ,  INOUE, Kenji

    IPC分类号： C07D319/06 ,  C07C69/675 ,  C07C69/716 ,  C12P7/42

    CPC分类号： C07D319/06 ,  C12P7/42 ,  C12P17/06

    摘要： A process for preparing optically active 2-[6-(hydroxy-methyl)-1,3-dioxan-4-yl]acetic acid derivatives which comprises reacting an enolate prepared by reacting an acetic acid ester derivative with a base or a zero-valent metal with (S)-β-hydroxy-η-butyrolactone at a temperature of -30°C or above to thereby obtain a dihydroxyoxohexanoic acid derivative, treating this derivative with an acylating agent in the presence of a base to thereby obtain a monoacylated derivative of dihydroxyoxohexanoic acid, reducing the monoacylated derivative with a microorganism into a monoacylated derivative of trihydroxyhexanoic acid, treating the resulting derivative with an acetal-forming reactant in the presence of an acid catalyst to thereby obtain an acyloxymethyldioxanylacetic acid derivative, and subjecting this derivative to solvolysis in the presence of a base.