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method for preparation of pharmaceutical preparations and methods for preparation of ergolinederivaten.

机译:药物制剂的制备方法和麦角灵碱的制备方法。

摘要

1505296 8-Thiomethylergoline derivatives ELI LILLY & CO 3 June 1975 [6 June 1974] 23869/75 Heading C2C Novel compounds of the Formula II wherein R is H, CN, COalk, phenyl or alk; RSP1/SP is H, Cl or Br; alk is C 1-3 alkyl and the dotted line is an optical bond and pharmaceuticallyacceptable acid addition salts thereof, may be prepared by reacting a compound of the Formula III wherein R 2 is methanesulphonyl or p-toluene sulphonyl with an alkali metal salt of a compound RSP3/SP5H, wherein RSP3/SP is CN, COalk, phenyl or alk, optionally followed where RSP3/SP is -COalk by hydrolysis to produce a compound II in which R is H. D - 6 - Methyl - 8 - mesyloxymethylergoline and its 9,10-didehydro derivative are prepared by reacting the corresponding 8-hydroxymethyl compound with methane sulphonyl chloride. Pharmaceutical compositions of the compounds II with the usual excipients are prolactin inhibitors when administered parenterally.
机译:1505296 8-硫代甲基麦角灵衍生物ELI LILLY&CO 1975年6月3日[1974年6月6日]标题C2C新型的式II化合物,其中R为H,CN,COalk,苯基或烷基; R 1 为H,Cl或Br; alk是C 1-3烷基,虚线是光学键及其药学上可接受的酸加成盐,可以通过使R 2为甲磺酰基或对甲苯磺酰基的式III化合物与α-的碱金属盐反应制得。化合物R 3 5H,其中R 3 是CN,COalk,苯基或烷基,可任选地随后通过水解来制备,其中R 3 是-COalk通过使相应的8-羟甲基化合物与甲烷磺酰氯反应,制得其中R是H的化合物Ⅱ。D-6-甲基-8-甲氧基甲基麦角灵及其9,10-二氢衍生物。肠胃外给药时,化合物Ⅱ与常用赋形剂的药物组合物是催乳激素抑制剂。

著录项

  • 公开/公告号NL180911B

    专利类型

  • 公开/公告日1986-12-16

    原文格式PDF

  • 申请/专利号NL19750006584

  • 发明设计人

    申请日1975-06-03

  • 分类号A61K31/48;C07D457/02;

  • 国家 NL

  • 入库时间 2022-08-22 07:20:07

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