Fu De-cai
2008
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Journal
Journal of Hebei Normal University
Abstract
The synthesis of 2,2-diphenyl-2-hydroxyacetic acid-1-methyl-4piperidinyl ester(4) was studied,which was an important intermediate and metabolite of propiverine hydrochloride.Reaction of 2,2-diphenyl-2-hydroxyacetate with enough methanol gave methyl ester in 95 % yield.Compound 4 was obtained by reaction of methyl 2,2-diphenyl-2-hydroxyacetate with 1-methyl-4-piperidinol in the mixture of toluene and methanol in the presence of metal sodium.The yield was 84.6 % and the purity of the product was higher than 99.0 %(HPLC).The chemical structure was confirmed by1H NMR and crystal structure was determined.