首页> 外国专利> method for preparing or manufacture of a product with a bronchodilatore - and / or platelet aggregation inhibitory effect and method for the processing of medicinal 6 prepare arylpyrimidineverbindingen, suitable for use in the former method.

method for preparing or manufacture of a product with a bronchodilatore - and / or platelet aggregation inhibitory effect and method for the processing of medicinal 6 prepare arylpyrimidineverbindingen, suitable for use in the former method.

机译:用于制备或生产具有支气管扩张剂和/或血小板聚集抑制作用的产品的方法以及用于加工药物的方法6制备芳基嘧啶verbindingen,适用于前一种方法。

摘要

1373536 4-Hydroxy-6-arylpyrimidines PFIZER Inc 4 Oct 1971 [5 Oct 1970] 38316/73 Divided out of 1373535 Heading C2C Novel 4-hydroxy-6-arylpyrimidines of the general formula wherein R 3 is a hydrogen atom or a C 1-3 alkyl group and Ar is a phenyl group (provided that R 3 is an ethyl group); a phenyl group monosubstituted by a fluorine, chlorine or bromine atom or a methyl, methoxy, hydroxy, trifluoromethyl, carboxy, cyano, nitro, di-C 1-3 alkylamino, amino or C 1-4 acylamino group; a 3,4-dimethoxyphenyl group; a pyridyl, thienyl or furyl group optionally monosubstituted by a C 1-4 acylamino group; or a naphthyl, 2- or 3-indolyl, 2- or 3-benzothienyl or 2- or 3-benzofuryl group, are prepared (a) by treatment of an ethyl 2-R 3 - 3-Ar-3-amino-acrylate with formamide in the presence of an alkali metal alkoxide; and (b) by reaction of an ethyl -ArCO--R 3 -acetate with thiourea and treatment of the resulting 2- mercapto-4-hydroxy-5-R 3 -6-Ar-pyrimidine with Raney nickel in aqueous sodium hydroxide. Pharmaceutical compositions having smooth muslce relaxant activity comprise, as active ingredient, 4-hydroxy-5-ethyl-6-phenylpyrimidine, together with a pharmaceutical carrier.
机译:1373536 4-羟基-6-芳基嘧啶PFIZER Inc 1971年10月4日[1970年10月5日]从1373535标题C2C中除掉通式为R 3为氢原子或C 1的新型4-羟基-6-芳基嘧啶-3个烷基,Ar为苯基(假设R 3为乙基);被氟,氯或溴原子或甲基,甲氧基,羟基,三氟甲基,羧基,氰基,硝基,二-C 1-3烷基氨基,氨基或C 1-4酰基氨基单取代的苯基; 3,4-二甲氧基苯基;吡啶基,噻吩基或呋喃基,其任选地被C 1-4酰基氨基单取代;或萘基,2-或3-吲哚基,2-或3-苯并噻吩基或2-或3-苯并呋喃基(a)通过处理2-R 3-3-Ar-3-氨基丙烯酸乙酯来制备在碱金属醇盐的存在下与甲酰胺一起; (b)使-ArCO-R 3-乙酸乙酯与硫脲反应,并用阮内镍在氢氧化钠水溶液中处理所得的2-巯基-4-羟基-5-R 3 -6-Ar-嘧啶。具有平滑的肌肉松弛活性的药物组合物包含4-羟基-5-乙基-6-苯基嘧啶作为活性成分以及药物载体。

著录项

  • 公开/公告号NL168511B

    专利类型

  • 公开/公告日1981-11-16

    原文格式PDF

  • 申请/专利权人 PFIZER INC. TE NEW YORK.;

    申请/专利号NL19710013670

  • 发明设计人

    申请日1971-10-05

  • 分类号C07D239/42;A61K31/395;A61K31/505;C07D239/36;C07D401/02;C07D405/04;C07D409/04;

  • 国家 NL

  • 入库时间 2022-08-22 13:43:49

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