Patent ID: 8097706
Filing Date: 2012-01-17
Classification: A61P,C07D,C07H,Y02P

Abstract:
1. A method for preparing capecitabine of formula 1, comprising the steps of: (1) hydrolyzing a methylacetonide compound of formula 2 to obtain a triol compound of formula 3; (2) reacting the compound of formula 3 with an haloalkyl formate of formula 4 in the presence of mixture of pyridine and triethylamine to obtain a β-anomer-rich trialkyl carbonate compound of formula 5; (3) conducting a glycosylation of the compound of formula 5 using 5-fluorocytosine in the presence of an acid to obtain a dialkoxycarbonyl cytidine compound of formula 6; (4) performing carbamoylation of the compound of formula 6 using n-pentyl chloroformate to obtain a carbamoylcytidine compound of formula 7; and (5) deprotecting the carbonate hydroxy protecting groups of the compound of formula 7: wherein, X is chloro, bromo or iodo; and R is methyl or ethyl.