PROCESSO PARA A OBTENCAO DE 3-<<2-{4-(6-FLUORO-BENZO-{D}-ISOXAZOL-3-IL)PIPERIDIN-1-IL}-ETIL>>-2-METIL-6,7,8,9-TETRA-HIDRO-4H-PIRIDO-{1,2-A}PIRIMIDIN-4-ONA

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 fo...

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Main Authors JOSE MARIA CALDERO GES, PERE DALMASES BARJOAN, JUAN HUGUET CLOTET, FRANCISCO MARQUILLAS OLONDRIZ, ANA BOSCH ROVIRA, JUAN CARLOS DEL CASTILLO NIETO
Format Patent
LanguagePortuguese
Published 30.01.2002
Edition7
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
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Summary: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.
Bibliography:Application Number: PT19950101654