首页> 外国专利> method for preparation of pharmaceutical preparations with anti arrhythmic activity, obtained by application of shaped products.and method for preparation of antiarrhythmic active 1 - cynnamil - 4 - benzhydrylpiperazine derivatives.

method for preparation of pharmaceutical preparations with anti arrhythmic activity, obtained by application of shaped products.and method for preparation of antiarrhythmic active 1 - cynnamil - 4 - benzhydrylpiperazine derivatives.

机译:成型产品获得的具有抗心律不齐活性的药物制剂的制备方法以及具有抗心律失常活性的1-氰基米尔-4-苯甲酰基哌嗪衍生物的制备方法。

摘要

1,268,710. Fluoro-substituted N-cinnamyl-NSP1/SP- benzhydryl piperazine. JANSSEN PHARMACEUTICA N.V. 10 June 1969 [2 July, 1968], No. 29382/69. Heading C2C. Novel fluoro-substituted N-cinnamyl-NSP1/SP- benzhydryl piperazines of the formula wherein each Ar may be a phenyl or fluorophenyl group, provided that at least one Ar is a fluorophenyl group, may be obtained by reacting a compound with a compound Y-CH 2 -CH=CH-Ar, where Y and YSP1/SP are different and represent a halogen atom or a piperazine residue, in the presence of a base and, if desired, forming a therapeutically active acid addition salt. Preparation of the following intermediates is also described: 1-(p-fluoro-.-phenylbenzyl)-piperazine from p-fluoro--phenylbenzylchloride and piperazine; p-fluorocinnamylchloride from pfluoro--vinylbenzyl alcohol and HCl; di-(4- fluorophenyl)-chloromethane from -(4-fluoro-phenyl)-4-fluorobenzyl alcohol and HCl. Pharmaceutical composition having anti-arrhythmic activity comprises a compound of Formula I above, or a therapeutically active acid addition salt thereof, in admixture with a pharmaceutically acceptable carrier, in forms suitable for oral or parenteral administration.
机译:1,268,710。氟取代的N-肉桂基-N 1 -苯甲基哌嗪。 JANSSEN PHARMACEUTICA N.V. 1969年6月10日[1968年7月2日],第29382/69号。标题C2C。下式的新型氟取代的N-肉桂基-N 1--二苯甲基哌嗪,其中每个Ar可以是苯基或氟苯基,条件是至少一个Ar是氟苯基,可以通过反应获得具有化合物Y-CH 2 -CH = CH-Ar的化合物,其中Y和Y 1 不同,并且在碱的存在下并且在需要时表示卤素原子或哌嗪残基,形成具有治疗活性的酸加成盐。还描述了以下中间体的制备:由对氟-苯基苄基氯和哌嗪的1-(对氟-.-苯基苄基)-哌嗪;来自对氟-乙烯基苄醇和HCl的对氟肉桂酰氯; -(4-氟-苯基)-4-氟苄醇和HCl中的二-(4-氟苯基)-氯甲烷。具有抗心律不齐活性的药物组合物包含以上式I的化合物或其治疗活性酸加成盐,与药学上可接受的载体混合,以适合口服或肠胃外给药的形式。

著录项

  • 公开/公告号NL6910007A

    专利类型

  • 公开/公告日1970-01-06

    原文格式PDF

  • 申请/专利权人

    申请/专利号NL19690010007

  • 发明设计人

    申请日1969-06-30

  • 分类号C07D51/70;A61K27/00;

  • 国家 NL

  • 入库时间 2022-08-23 11:33:50

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