http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1280804-A1

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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-18
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04
filingDate 2000-05-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_89f2865ee74d8e055eafc7ce5cdb573b
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fb5a5d935dd3036bd48415cfe3c6b6a2
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publicationDate 2003-02-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-1280804-A1
titleOfInvention A process for the preparation of anti-pschotic 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
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.
priorityDate 2000-05-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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