The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Dec. 11, 2007

Filed:

Nov. 13, 2002
Applicants:

László Pongó, Kerepes, HU;

József Reiter, Budapest, HU;

Gyula Simig, Hudapest, HU;

Gábor Berecz, Budapest, HU;

György Clementis, Budapest, HU;

Péter Slégel, Budapest, HU;

János Szulágyi, Budapest, HU;

László Koncz, Mogyoród, HU;

Györgyi Vereczkeyné Donáth, Budapest, HU;

Kálmán Nagy, Budapest, HU;

Gyuláné Körtvélyessy, Budapest, HU;

Inventors:

László Pongó, Kerepes, HU;

József Reiter, Budapest, HU;

Gyula Simig, Hudapest, HU;

Gábor Berecz, Budapest, HU;

György Clementis, Budapest, HU;

Péter Slégel, Budapest, HU;

János Szulágyi, Budapest, HU;

László Koncz, Mogyoród, HU;

Györgyi Vereczkeyné Donáth, Budapest, HU;

Kálmán Nagy, Budapest, HU;

Gyuláné Körtvélyessy, Budapest, HU;

Assignee:

EGIS Gyógyszergyár Rt., Budapest, HU;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 239/70 (2006.01);
U.S. Cl.
CPC ...
Abstract

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.


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