FIELD: chemistry.
SUBSTANCE: present invention relates to method of producing capecitabine involving the following steps: 1) hydrolysis of a methylacetonide compound to obtain a triol compound of formula , 2) reaction of the triol compound with haloalkyl formate of the given formula in the presence of a mixture of pyridine and triethylamine to obtain a β-anomer rich trialkylcarbonate compound of formula , 3) glycosylation of the trialkylcarbonate compound using 5-fluorocytosine in the presence of an acid, 4) carbamylation of the obtained compound of formula using n-pentylchloroformate, followed by 5) removal of carbonate hydroxy-protective groups of the furan ring.
EFFECT: efficient method of obtaining capecitabine.
7 cl, 4 ex
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Authors
Dates
2012-01-10—Published
2008-11-07—Filed