Process for the preparation of 3-{2-'4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyllethyl}-6,7,8,9-tetrahydro--2-methyl-4h-pyrido'1,2-methyl-4h-pyrido',2-a!pyrimidin-4-one

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United States of America Patent

PATENT NO 7307168
APP PUB NO 20050004141A1
SERIAL NO

10495362

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Abstract

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The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tet-rahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by subjecting the oxime of the Formula (II), to ring-closure in the presence of an alkali hydroxide, alkali carbonate or alkali-C.sub.1-4 alkoxide in an inert organic solvent, converting the base of the Formula I thus obtained into an acid addition salt or setting free the base of the Formula I from an acid addition salt thereof which comprises reacting a halogen derivative of the general Formula (XIV), (wherein Hal is halogen) with piperidine oxime derivative of the Formula (V), or an acid addition salt thereof in the presence of a base, and using by the ring-closure of the oxime of the Formula II formed a C.sub.1-4-alkanol as inert solvent. The process of the present invention enables the economical preparation of a product having a purity suitable for pharmaceutical purposes.

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Patent Owner(s)

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EGIS GYOGYSZERGYAR RTBUDAPEST BUDAPEST BUDAPEST

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Berecz, Ga Budapest, HU 1 1
Clementis, Gyo Budapest, HU 1 1
Donath, Gyoe Budapest, HU 1 1
Koncz, Lao Mogyorod, HU 1 1
Kortvelyessy, Gyulae Budapest, HU 1 1
Nagy, Kaa Budapest, HU 1 1
Pongo, Lao Kerepes, HU 1 1
Reiter, Jo Budapest, HU 1 1
Simig, Gyula Hudapest, HU 75 181
Slegel, Pe Budapest, HU 1 1
Szulagyi, Ja Budapest, HU 1 1

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