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Regioselective enzymatic synthesis of non-steroidal anti-inflammatory drugs containing glucose in organic media.

作者信息

Wang Na, Liu Bo Kai, Wu Qi, Wang Jun Liang, Lin Xian Fu

机构信息

Department of Chemistry, Zhejiang University, 310027, Hangzhou, P.R. China.

出版信息

Biotechnol Lett. 2005 Jun;27(11):789-92. doi: 10.1007/s10529-005-5799-2.

DOI:10.1007/s10529-005-5799-2
PMID:16086261
Abstract

Enzymatic transesterification of glucose with the vinyl ester of non-steroidal anti-inflammatory drugs (NSAIDs) was in organic media performed for synthesis of novel NSAIDs-glucose conjugates. Glucose was regioselectively acylated at the 6-hydroxyl group. The indomethacin-glucose conjugate and ketoprofen-glucose conjugate were produced by the catalysis of alkaline protease from Bacillus subtilis in the respective yields of 42% (over 48 h) and 63% (over 40 h). The etodolac-glucose conjugate was obtained in 26% yield (over 144 h) by lipase from Candida antarctica.

摘要

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