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    Process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives
    5.
    发明授权
    Process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives 有权
    光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的制备方法

    公开(公告)号：US06903225B2

    公开(公告)日：2005-06-07

    申请号：US10242453

    申请日：2002-09-13

    Applicant: Noriyuki Kizaki ,  Yukio Yamada ,  Yoshihiko Yasohara ,  Akira Nishiyama ,  Makoto Miyazaki ,  Masaru Mitsuda ,  Takeshi Kondo ,  Noboru Ueyama ,  Kenji Inoue

    Inventor： Noriyuki Kizaki ,  Yukio Yamada ,  Yoshihiko Yasohara ,  Akira Nishiyama ,  Makoto Miyazaki ,  Masaru Mitsuda ,  Takeshi Kondo ,  Noboru Ueyama ,  Kenji Inoue

    IPC: C07C67/343 ,  C07C253/30 ,  C07C255/21 ,  C07D319/06 ,  C12P7/62 ,  C12P1/04 ,  C12P17/06

    CPC classification number: C07D319/06 ,  C07B2200/07 ,  C07C67/343 ,  C07C253/30 ,  C12P7/62 ,  C07C69/716 ,  C07C255/21

    Abstract: 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 halomethyl-dioxanylacetic 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.

    Abstract translation: 本发明提供了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的2- [6-（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 例如超低温反应所需的。 一种制备光学活性的2- [6-（羟基甲基）-1,3-二恶烷-4-基]乙酸衍生物的方法，其包括使不饱和-30℃的乙酸衍生物与烯醇化物 通过使碱金属或0价金属作用于衍生物以制备羟基己酸衍生物而制备，借助于微生物菌株还原该化合物以提供卤代甲基二恶烷基乙酸衍生物，用缩醛化处理该化合物 在酸催化剂存在下，提供卤代甲基 - 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。

    Medicinal use of n-phenyl-2-cyano-3-hydroxycrotonamide derivatives
    8.
    发明授权
    Medicinal use of n-phenyl-2-cyano-3-hydroxycrotonamide derivatives 失效
    N-苯基-2-氰基-3-羟基巴豆酰胺衍生物的药用

    公开(公告)号：US5773470A

    公开(公告)日：1998-06-30

    申请号：US902626

    申请日：1997-07-29

    Applicant: Rudolf Schleyerbach ,  Robert Ryder Bartlett ,  Elizabeth Anne Kuo ,  Edward James Little

    Inventor： Rudolf Schleyerbach ,  Robert Ryder Bartlett ,  Elizabeth Anne Kuo ,  Edward James Little

    IPC: C07C255/30 ,  A61K31/16 ,  A61K31/275 ,  A61K31/277 ,  A61P29/00 ,  A61P37/00 ,  A61P37/06 ,  C07C253/00 ,  C07C255/20 ,  C07C255/21 ,  C07C255/23 ,  C07C255/27 ,  C07C323/36

    CPC classification number: A61K31/277 ,  A61K31/275 ,  C07C255/23

    Abstract: N-Phenyl-2-cyano-3-hydroxycrotonamide derivatives and their use as pharmaceuticals having an immunomodulatory property. The use of N-phenyl-2-cyano-3-hydroxycrotonamide derivatives of the formula I ##STR1## in which R.sup.1 is a hydrogen atom or (C.sub.1 -C.sub.4)-alkyl, R.sup.2 is CN, CX.sub.3, WCX.sub.3, W(CH.sub.2).sub.n CX.sub.3, NO.sub.2, (CH.sub.2).sub.n CX.sub.3, or halogen, in which X is halogen, W is an oxygen or sulfur atom and n is an integer from 1 to 3, R.sup.3 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, CN or --CO--R.sup.4, in which R.sup.4 is (C.sub.1 -C.sub.4)-alkyl or (C.sub.3 -C.sub.6)-cycloalkyl, and/or their physiologically tolerable salts, for the treatment of rheumatic diseases, autoimmune diseases, and of rejection reactions of the organ recipient to the transplanted organ, is described.

    Abstract translation: N-苯基-2-氰基-3-羟基巴豆酰胺衍生物及其作为具有免疫调节性的药物的用途。 使用式I C 1 -C 4） - 烷基，R 2的N-苯基-2-氰基-3-羟基巴豆酰胺衍生物是CN，CX3，WCX3，W（CH2）nCX3，NO2，（CH2）nCX3或卤素， 其中X是卤素，W是氧或硫原子，n是1-3的整数，R3是（C1-C4） - 烷基，（C3-C6） - 环烷基，CN或-CO-R4，其中 R4是用于治疗风湿性疾病，自身免疫疾病和器官受体对移植器官的排斥反应的（C 1 -C 4） - 烷基或（C 3 -C 6） - 环烷基和/或其生理上可耐受的盐，是 描述。

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