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110 条记录 (耗时 0.017 秒)

    Preparation of prostaglandin f
    1.
    发明专利
    Preparation of prostaglandin f 失效
    PROSTAGLANDIN F的制备

    公开(公告)号：JPS5942364A

    公开(公告)日：1984-03-08

    申请号：JP15281082

    申请日：1982-09-03

    申请人： Teijin Ltd

    发明人： SUGIURA SATOSHI ,  SAKAUCHI KIYOSHI ,  YUU TAKESHI ,  KUROZUMI SEIJI

    IPC分类号： C07C405/00 ,  C07C67/00 ,  C07C401/00

    摘要： PURPOSE: To obtain the titled compound useful as a labor pain promotor or intestinal hyperkinetic agent, etc. from an easily available raw material in high yield in short step, by reducing a 7-sulfonyloxyprostaglandin F.
    CONSTITUTION: A 7-sulfonyloxyprostaglandin F of formula I (B is -CH
    2 -CH
    2 , -CH=CH- or -C≡C-,; R
    1 is H, 1W10C alkyl, phenyl or cycloalkyl, etc.; R
    2 is 1W14C alkyl, phenyl, etc.; R
    3 and R
    4 are H, OH, etc.; R
    5 is unsubstituted 1W 8C alkyl, phenyl, etc.; R
    6 is H, methyl, ethynyl, etc.; the dotted line part is a single or double bond) is reduced with a reducing reaction agent, e.g. sodium boron hydride, in a solvent, e.g. hexamethylphosphoric triamide or dimethyl sulfoxide, at 0W150°C, preferably 30W100°C, to give the aimed substance of formula II.
    COPYRIGHT: (C)1984,JPO&Japio

    摘要翻译： 目的：通过减少7-磺酰氧基前列腺素F，从短容易地获得的原料中获得用作劳动疼痛促进剂或肠肌运动剂等的标题化合物。构成：式7的7-磺酰氧基前列腺素F I（B是-CH 2 -CH 2，-CH = CH-或-C≡C），R 1是H，1-10C烷基，苯基或环烷基等; R 2是1-14C烷基，苯基 等; R 3和R 4是H，OH等; R 5是未取代的1- 8C烷基，苯基等; R 6是H，甲基，乙炔基等。 ;虚线部分是单键或双键）用还原反应剂还原，例如 硼氢化钠。 六甲基磷酰三胺或二甲基亚砜，在0-150℃，优选30-100℃，得到式II的目标物质。

    PREPARATION OF FLUORO-PGI2
    2.
    发明专利
    PREPARATION OF FLUORO-PGI2 失效

    公开(公告)号：JPS5867682A

    公开(公告)日：1983-04-22

    申请号：JP16420081

    申请日：1981-10-16

    申请人： TEIJIN LTD

    发明人： SAKAUCHI KIYOSHI ,  YUU TAKESHI ,  OOBA TAKEO ,  TANAKA TOSHIO ,  OKAMURA NORIAKI ,  WATANABE KENZOU ,  KUROZUMI SEIJI ,  OOTSU AKIRA ,  NARITOMO TATSUYUKI

    IPC分类号： C07D307/935 ,  C07F7/18

    摘要： PURPOSE:To prepare the titled compound having high stability and useful as a remedy for thrombosis, a hypotensor, etc., from an easily available raw material, by reacting a specific 5-halo-DELTA -PGI1 with a fluorination reagent such as a metal fluoride, etc. CONSTITUTION:The objective compound of formula II (R is H or 1-10C alkyl; R and R are H or OH-protecting group; R is fluorine atom and R and R together form a single bond, or R is fluorine atom and R and R together form a single bond) can be prepared by reacting the 5-halo-DELTA -PGI1 of formulaI(R is H or 1-10C alkyl; R and R are H or OH-protecting group; X is Cl, Br or I) (e.g. 5-bromo-DELTA -PGI1 methyl ester 11,15-diacetate) with a fluorinating reagent such as a metal fluoride (e.g. silver fluoride) in a solvent such as acetonitrile.

    NOVEL VINYL ETHER DERIVATIVE AND ITS PREPARATION
    6.
    发明专利
    NOVEL VINYL ETHER DERIVATIVE AND ITS PREPARATION 失效

    公开(公告)号：JPS5663979A

    公开(公告)日：1981-05-30

    申请号：JP13938579

    申请日：1979-10-30

    申请人： TEIJIN LTD

    发明人： TANAKA TOSHIO ,  YUU TAKESHI ,  OOBA TAKEO ,  OKAMURA NORIAKI ,  WATANABE KENZOU ,  SAKAUCHI KIYOSHI ,  KUROZUMI SEIJI

    IPC分类号： C07D307/935 ,  A61K31/34 ,  A61K31/343 ,  A61P43/00

    摘要： NEW MATERIAL:A compound of formula I (R 1 and R2 are H or protecting group; Y is H; X is halogen, or X and Y together form a C-C bond). EXAMPLE:1,2,3,4-Tetranor-prostaglandin I2. USE:An intermediate for the production of a prostaglandin I2 analogue having blood platelet coagulation inhibiting, coagulated platelet dissolving, arterial duct relaxing, and hypotensive activities, etc. PROCESS:A compound of formula I wherein Y is H and X is halogen is prepared by the halogenative cyclization of a compound of formula II with a reaction reagent such as N-bromosuccinimide, etc. The compound thus prepared is converted to another compound of formula I wherein X and Y together form a C-C bond by reacting with an organic base, e.g. 1,5-diazabicyclo[5,4,0]undecene-5, in an organic solvent such as benzene at 0-150 deg.C, and subjecting the product to dehydrohalogenation reaction.