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6-(2-Aminoethylamino)-1,2,4-triazolo-(3,4-a)-phthalazine derivs.

机译:6-(2-氨基乙基氨基)-1,2,4-三唑-(3,4-a)-酞嗪衍生物。

摘要

Cpds. of the formula (I) and their acid addition salts are new, (where R is H or (1-4C)alkyk; m is 0 or 1; n is 4 or 5). In an example, mixture of 6-chloro-7,8,9,10 -tetrahydro-1,2,4 -triazolo(3,4-a)phthalazine (5.0g), 1-(2-aminoethyl) pyrrolidine (10.0g) and 2-methoxyethanol (50 ml) was refluxed for 15 hrs., concentrated, and partitioned between CH2Cl2 and satd. aq. NaHCO3 soln. The organic layer was dried, concentrated, triturated with ether and filtered to give 6-(2-(1-pyrrolidinyl) ethylamino)-7,8,9,10 -tetrahydro-1,2,4-triazolo (3,4-a)phthalazine (m.pt. 160-162 deg. C). (0/0) EPAB- EP-104506 B A compound of formula (I)wherein R is hydrogen or alkyl of 1-4 carbon atoms; m is 0 or 1; and n is 4 or 5; and the pharmaceutically acceptable acid addition salts thereof. - (12pp) USAB- US4487930 A 6-((Cyclic amino)alkoxyamino) -tetrahydrotriazolo (3,4-a)phthalazine cpds. of formula (I) and their salts are new. In the formula, R is H or 1-4C alkyl m is 0 or 1 n is 4 or 5. The cpds. can be prepd. by reacting a 6-halo 7,8,9,10-tetrahydro -1,2,4-triazolo (3,4-a)phthalazine with an amine of formula (II).
机译:Cpds。式(I)的式(I)及其酸加成盐是新的(其中R为H或(1-4C)烷基; m为0或1; n为4或5)。在一个实例中,是6-氯-7,8,9,10-四氢-1,2,4-三唑并(3,4-a)邻苯二甲酸(5.0g),1-(2-氨基乙基)吡咯烷(10.0)的混合物g)和2-甲氧基乙醇(50ml)回流15小时,浓缩,并在CH 2 Cl 2和饱和NaHCO 3之间分配。水NaHCO3溶液。干燥有机层,浓缩,用乙醚研磨并过滤,得到6-(2-(1-(吡咯烷基)乙基氨基)-7,8,9,10-四氢-1,2,4-三唑(3,4- a)酞嗪(熔点:160-162℃)。 (0/0)EPAB-EP-104506 B一种式(I)的化合物,其中R是氢或1-4个碳原子的烷基; m为0或1; n为4或5;及其药学上可接受的酸加成盐。 -(12pp)USAB- US4487930 A 6-((环氨基)烷氧基氨基)-四氢三唑(3,4-a)邻苯二甲酰cpds。式(I)的化合物及其盐是新的。式中,R为H或1-4C烷基,m为0或1 n为4或5。可以准备。使6-卤代7,8,9,10-四氢-1,2,4-三唑(3,4-a)酞嗪与式(II)的胺反应。

著录项

  • 公开/公告号ES8601985A1

    专利类型

  • 公开/公告日1986-03-01

    原文格式PDF

  • 申请/专利权人 THE DOW CHEMICAL COMPANY.;

    申请/专利号ES19830525368

  • 发明设计人

    申请日1983-09-05

  • 分类号C07D457/04;A61K31/395;C07D403/14;

  • 国家 ES

  • 入库时间 2022-08-22 07:37:41

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