Ji Ya-fei
2010
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Journal
Chinese Journal of Pharmaceuticals
Abstract
2-Amino-3-hydroxypyridine reacted with benzyl chloride to give 2-amino-3-benzyloxypyridine(3),which was cyclized with α-acetyl-γ-butyrrolactone to provide 9-benzyloxy-3-(2-hydroxyethyl)-2-methyl-4H-pyrido[1,2a]pyrimidin-4-one(4).Compound 4 underwent chlorination,reduction and debenzylation to afford the key intermediate 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one(6).Finally,compound 6 was subjected to nucleophilic substitution with 6-fluoro-3-(4-piperidinyl)-1,2-benzoisoxazol hydrochloride to achieve the title product paliperidone with an overall yield of about 35%.