Process for the preparation of anti-psychotic...

Details Process for the preparation of anti-psychotic... Process for the preparation of anti-psychotic...

2005-05-24

2005-05-24

Raymond, Richard L. (Department: 1624)

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

Reexamination Certificate

active

06897308

ABSTRACT:
A process for the preparation of 3-substituted ethyl-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2,-a]pyrimidin-4-one of the formula IIB:where X may be halo, acyloxy, or sulfonyloxy such as tosyloxy or mesyloxy, an intermediate in the synthesis of the anti-psychotic risperidone. The process comprises hydrogenation of 3-substituted ethyl-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one in aqueous inorganic acid medium at atmospheric to 60 psi at 0-100° C. in the presence of a metal catalyst and the product is isolated. A process for the preparation of risperidone of the formula I:comprising condensation of 3-substituted ethyl-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2,-a]pyrimidin-4-one with 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole in water in the presence of an inorganic base at 25-100° C. and the product is isolated.

REFERENCES:
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patent: 4957916 (1990-09-01), Kennis et al.
patent: 5015740 (1991-05-01), Kennis et al.
patent: 0196132 (1986-10-01), None
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patent: 2074966 (1995-09-01), None
English Language Abstract for Spainish Appln. No. 2074966, 1995.
“Synthesis of Drugs & Drug Intermediates” submitted to “The University of Mumbai” by Ms. Evelyn D. Lobo, Jun. 1996.

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