Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...
Reexamination Certificate
2007-12-11
2007-12-11
Shameem, Golam M. M. (Department: 1626)
Organic compounds -- part of the class 532-570 series
Organic compounds
Nitrogen attached directly or indirectly to the purine ring...
C544S224000, C544S242000, C544S245000, C544S253000
Reexamination Certificate
active
10495362
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-C1-4alkoxide 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 C1-4-alkanol as inert solvent. The process of the present invention enables the economical preparation of a product having a purity suitable for pharmaceutical purposes.
REFERENCES:
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patent: 5658916 (1997-08-01), Caldero Ges et al.
patent: 6897308 (2005-05-01), Venkatasubramanian et al.
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Marquillas et al (1994): STN International HCAPLUS database, Columbus (Ohio), accession No. 1994:655824.
Berecz Gábor
Clementis Gyōrgy
Donáth Györgyi Vereczkeyné
Koncz László
Körtvélyessy Gyuláné
EGIS Gyógyszergyár Rt.
Shameem Golam M. M.
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