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Process for the preparation of new derivatives of Burgo (b) tiophéine.

机译:制备Burgo(b)噻吩的新衍生物的方法。

摘要

1357212 Benzothiapine derivatives LABAZ 16 June 1972 [25 June 1971] 30032/71 Heading C2C Novel compounds of Formula I and the pharmaceutically acceptable acid addition salts thereof, for example the oxalate or hydrochloride, wherein R represents hydrogen or a branched or straight-chain alkyl group containing from 1 to 4 carbon atoms, RSP1/SP represents hydrogen or methyl, X and X 1 , which are identical, each represent an atom of chlorine, bromine or iodine, Am represents a dimethylamino, diethylamino, di - n - propylamino, di - n - butylamino, pyrrolidino, piperidino or perhydroazepino group, and n is an integer in the range of from I to 5 inclusive are prepared by reaction of HAm with a compound of Formula IV or in the case where n is 1 or 2 by reaction of a compound II with (Z is halogen or tosyloxy). Intermediates of Formula IV above are prepared by reaction of with an intermediate of Formula II above obtained by the demethylation of the corresponding methyl ether starting material followed by halogenation. Pharmaceutical compositions in conventional forms for oral or rectal administration comprise an above novel compound and a carrier or diluent. The compositions are of use in the treatment of heart conditions.
机译:1357212苄硫平衍生物LABAZ 1972年6月16日[1971年6月25日] 30032/71标题C2C新型的式I化合物及其药学上可接受的酸加成盐,例如草酸盐或盐酸盐,其中R代表氢或支链或直链烷基含1-4个碳原子的基团,R 1 代表氢或甲基,X和X 1相同,分别代表氯,溴或碘原子,Am代表二甲氨基,二乙氨基,通过使HAm与式IV的化合物反应或在以下情况下制备二正丙基氨基,二正丁基氨基,吡咯烷基,哌啶子基或全氢氮杂环庚烷基,并且n为I至5的整数。通过化合物II与(Z为卤素或甲苯磺酰氧基)反应,n为1或2。通过与相应的甲醚原料进行去甲基化然后卤化而获得的上述式II的中间体反应来制备上述式IV的中间体。用于口服或直肠给药的常规形式的药物组合物包含上述新型化合物和载体或稀释剂。该组合物可用于治疗心脏疾病。

著录项

  • 公开/公告号OA04117A

    专利类型

  • 公开/公告日1979-11-30

    原文格式PDF

  • 申请/专利权人 LABAZ S.A.;

    申请/专利号OA19720054619

  • 发明设计人 DESCAMPS MARCEL;CLAEYS NORBERT;

    申请日1972-06-26

  • 分类号C07D333/56;

  • 国家 OA

  • 入库时间 2022-08-22 18:25:22

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