Process for preparation of...

Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...

Reexamination Certificate

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Reexamination Certificate

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08071767

ABSTRACT:
Described herein is an improved, commercially viable and industrially advantageous process for the preparation of paliperidone intermediate 9-hydroxy-3-(2-chloroethyl)-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one and its hydrochloride salt. The process provides the paliperidone intermediate in higher yield and reduced reaction time compared to the previously disclosed processes, thereby providing for production of paliperidone and its pharmaceutically acceptable acid addition salts in high purity and in high yield.

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Kennis, et. al., Bioorganic & Medicinal Chemistry Letters (2000), 10(1), 71-74.
International Search Report and Written Opinion; International Application No. PCT/IB2008/000626; International Filing Date Jan. 8, 2008; Date of Mailing: Dec. 18, 2008; 16 pages.
DeSMET, et al.; “Selectivity Control by Use of Near-IR for a Hydrogenation Process”; Organic Process Research & Development; 9; pp. 344-347; (2005).
Badawey, et. al.; “Synthesis of Some New Imidazo[1,2-a]pyrimidin-5(1H)-ones as Potential Antineoplastic Agents”; Journal of Heterocyclic Chemistry; 32; pp. 1003-1006; (1995).

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