首页> 外国专利> 3- (6-FLUORO-BENZO- (D) -ISOXAZOL-3-YL) PIPERIDIN-1-YL} -ETHYL -2-METHYL-6,7, 8,9-TETRAHYDRO-4H-PYRIDO- {1,2-A} PYRIMIDIN-4-ONA

3- (6-FLUORO-BENZO- (D) -ISOXAZOL-3-YL) PIPERIDIN-1-YL} -ETHYL -2-METHYL-6,7, 8,9-TETRAHYDRO-4H-PYRIDO- {1,2-A} PYRIMIDIN-4-ONA

机译:3-(6-氟-苯并-(D)-异恶唑-3-基)哌啶-1-基}-乙基] -2-甲基-6,7,8,9-四氢-4H-吡啶基-{1, 2-A} PYRIMIDIN-4-ONA

摘要

Process for obtaining 3-2-[4-(6-fluoro-benzo[d]isoxazol-3- yl)-piperidin-1-yl]-ethyl-2-methyl-6,7,8,9-tetrahydro-4H- pyrido-[1,2-a]pyrimidine-4-one The process comprises reacting 3-(2-aminoethyl)-2-methyl- 6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine-4-one of formula II with compounds of general formula III where Y and Z are projecting groups which may be the same or different such as halogen or an alkyl or aryl sulphonyloxy group in the presence of an appropriate solvent and base to provide 3-2-[4-6-fluoro- benzo[d]isoxazol-3-yl)piperidin-I-yl]-ethyl-2-methyl- 6,7,8,9-tetrahydro-4Hpyrido [1,2-a] pyrimidine-4-one of general formula I. The said compound has pharmaceutical applications on account of its antipsychotic properties. Products of formulae II and III which are necessary for the performance of this invention are also claimed.
机译:获得3-2- [4-(6-氟-苯并[d]异恶唑-3-基)-哌啶-1-基]-乙基-2-甲基-6,7,8,9-四氢-4H的方法-吡啶基-[1,2-a]嘧啶-4-酮该方法包括使3-(2-氨基乙基)-2-甲基-6,7,8,9-四氢-4H-吡啶[1,2-a反应在适当的溶剂和碱存在下,通式II的] pyrimidine-4-one与通式III的化合物一起使用,其中Y和Z是伸出的基团,它们可以相同或不同,例如卤素或烷基或芳基磺酰氧基3-2- [4-6-氟-苯并[d]异恶唑-3-基)哌啶-1-基]-乙基-2-甲基-6,7,8,9-四氢-4吡啶基[1,2- a]通式I的嘧啶-4-酮。所述化合物由于其抗精神病特性而具有药学应用。还要求保护对于实现本发明而言必要的式II和III的产物。

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