Egis Gyogyszergyar Rt.

Egis Gyogyszergyar Nyilvanosan Mukodo Reszvenytarsasag

József Reiter

Kálmán Nagy

Györgyi Vereczkeyné Donáth

László Pongó

Gyula Simig

Tibor Mezei

Ferenc Lorant Bartha

Péter Trinka

János Szulágyi

Gyuláné Körtvélyessy

Gábor Berecz

György Clementis

Zoltán Katona

Péter Slégel

László Koncz

Donáth Györgyi Vereczkeyné

According to the present invention, 2-chloroethoxy-acetic acid-N,N-dimethylamide of the Formula (I) is prepared by reacting 2-hydroxyethoxy-acetic acid-N,N-dimethylamide of the Formula (II) in a solvent optionally in the presence of a catalyst with thionyl chloride and removing the solvent by distillation. 

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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-tetrahydro-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-Calkoxide 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-alkanol as inert solvent. The process of the present invention enables the economical preparation of a product having a purity suitable for pharmaceutical purposes.

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&#x2032;1,2-methyl-4h-pyrido&#x2032;,2-a!pyrimidin-4-one

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Budapest, Hungary

József Reiter