PROCESS FOR PRODUCING 3-{2-[4-(6-FLUORO-BENZO[D]ISOXAZOL-3-YL)PIPERIDINE-1-IL]-ETHYL}-2-METHYL-6,7,8,9-TETRAHYDRO-4H-PYRIDO[1,2-A]PYRIMIDINE-4-ONE AND INTERMEDIATES

• Main Authors: DEL CASTILLO NIETO, JUAN CARLOS, BOSCH ROVIRA, ANA, CALDERO GES, JOSE MARIA, HUGUET CLOTET, JOAN, DALMASES BARJOAN, PERE, MARQUILLAS OLONDRIZ, FRANCISCO
• Format: Patent
• Language: English; Hungarian
• Published: 28.04.2003
• Edition: 7
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

A találmány tárgya új eljárás az (I) képletű 3-{2-[4-(6-fluor-benzo[d]izoxazol-3-il)-piperidin-1-il]-etil}-2-metil-- 6,7,8,9-tetrahidro-4H-pirido[1,2-a]pirimidin-4-on előállítására. A találmányszerint olyan módon járnak el, hogy 3-(2-amino-etil)-2-metil-6,7,8,9-tetrahidro-4H-pirido[1,2-a]pirimi- din-4-on-vegyületet egybenzoizoxazolszármazékkal reagáltatnak. A találmány tárgyát képeziktovábbá az új 3-{2-[4-(6-fluor-benzo[d]izoxazol-3-il)-piperidin-1-il]-etil}-2-metil-- 6,7,8,9-tetrahidro-4H-pirido[1,2-a]pirimidin-4-on ésbenzoizoxazolszármazék intermedierek is. ŕ 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.