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    • 10. 发明专利
    • Preparation of homopiperazine derivative
    • 双酚A衍生物的制备
    • JPS5948467A
    • 1984-03-19
    • JP15883782
    • 1982-09-14
    • Nisshin Flour Milling Co LtdNisshin Kagaku Kk
    • KIKUCHI HARUHIKO
    • C07D243/08A61K31/55A61P9/08A61P9/10B01J29/06B01J31/02C07B61/00C07D243/06
    • Y02P20/52
    • PURPOSE: To prepare the titled compound, in high yield, by the ester-exchange of N,N'-bis(3-hydroxypropyl)homopiperazine with a 3,4,5-trimethoxybenzoic acid ester under basic condition while removing the produced lower alcohol.
      CONSTITUTION: The homopiperazine derivative of formula III {e.g. N,N'-bis[3- (3',4',5'-trimethoxybenzoyloxy)propyl]homopiperazine} is prepared by the ester- exchange reaction of the N,N'-bis(3-hydroxypropyl)-homopiperazine of formula I with the 3,4,5-trimethoxybenzoic acid ester of formula II (R is lower alkyl) in the presence of a base (e.g. sodium ethoxide) while absorbing and removing the by-produced lower alcohol from the system with a molecular sieve.
      USE: A drug having coronary vessel dilating activity.
      COPYRIGHT: (C)1984,JPO&Japio
    • 目的:通过在碱性条件下,通过N,N'-双(3-羟丙基)高哌嗪与3,4,5-三甲氧基苯甲酸酯的酯交换,高产率制备标题化合物,同时除去产生的低级醇 。 构成:式III的高哌嗪衍生物(例如, N,N'-双[3-(3',4',5'-三甲氧基苯甲酰氧基)丙基]高哌嗪}是通过式(I)的N,N'-双(3-羟丙基) - 高密度哌嗪的酯交换反应 I在碱(例如乙醇钠)存在下与式II的3,4,5-三甲氧基苯甲酸酯(R是低级烷基),同时用分子筛吸收并除去副产物的低级醇。 使用:具有冠状血管扩张活性的药物。