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利巴韦林的区域选择性酶促酰化反应以制备潜在的多功能衍生物。

Regioselective enzymatic acylation of ribavirin to give potential multifunctional derivatives.

作者信息

Liu Bo-Kai, Wang Na, Wu Qi, Xie Chuan-Ying, Lin Xian-Fu

机构信息

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

出版信息

Biotechnol Lett. 2005 May;27(10):717-20. doi: 10.1007/s10529-005-5188-x.

Abstract

Lipase-catalyzed synthesis of potential multifunctional ribavirin derivatives was performed in acetone. Divinyl dicarboxylates with different chain lengths (C4, C6, C9, C10) were used as acyl donors and the reactions were catalyzed by lipase immobilized on acrylic resin from Candida antarctica (CAL-B). Ribavirin was regioselectivly acylated at the primary hydroxyl groups and the corresponding vinyl esters (C4, C6, C9, C10) were prepared in respective yields of 48%, 65%, 54%, 55%.

摘要

在丙酮中进行脂肪酶催化合成潜在的多功能利巴韦林衍生物。使用具有不同链长(C4、C6、C9、C10)的二乙烯基二羧酸酯作为酰基供体,反应由固定在南极假丝酵母丙烯酸树脂上的脂肪酶(CAL-B)催化。利巴韦林在伯羟基上进行区域选择性酰化,相应的乙烯基酯(C4、C6、C9、C10)的产率分别为48%、65%、54%、55%。

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