METHOD OF PRODUCING CAPECITABINE AND β-ANOMER RICH TRIALKYLCARBONATE COMPOUND USED THEREIN Russian patent published in 2012 - IPC C07D239/36 C07D307/20 C07D307/22 C07D405/04 

Abstract RU 2439064 C1

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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RU 2 439 064 C1

Authors

Li Dzaekheon

Park Ga-Seung

Jang Veon Ki

Kim Dzin Khi

Park Cheol Khiun

An Jong-Khoon

Li Joon Dzu

Chang Jang-Kil

Li Gvan Sun

Dates

2012-01-10Published

2008-11-07Filed