由糖聚合物-酶共轭物催化的9-(2,3-二羟基丙基)腺嘌呤的区域选择性棕榈酰化
Regioselective Palmitoylation of 9-(2,3-Dihydroxy- propyl)adenine Catalyzed by a Glycopolymer-enzyme Conjugate.
作者信息
Brabcová Jana, Blažek Jiří, Krečmerová Marcela, Vondrášek Jiří, Palomo Jose M, Zarevúcka Marie
机构信息
Institute of Organic Chemistry and Biochemistry, AS CR, Flemingovo nám. 2, Prague 6, Czech Republic.
Departamento de Biocatálisis, Instituto de Catálisis (CSIC) Campus UAM Cantoblanco, Madrid 28049, Spain.
出版信息
Molecules. 2016 May 16;21(5):648. doi: 10.3390/molecules21050648.
The enzymatic regioselective monopalmitoylation of racemic 9-(2,3-dihydroxypropyl)- adenine (DHPA), an approved antiviral agent, has been performed by an immobilized form of Candida antarctica B lipase (CAL-B) using a 4:1 DMF/hexane mixture as the reaction medium. To improve the chemical yield of the desired monopalmitoylation reaction, solid-phase chemical modifications of the lipase were evaluated. The reaction yield was successfully increased obtaining 100% product after a second treatment of the product solution with fresh immobilised chemically glycosylated-CAL-B.
已使用固定化的南极假丝酵母脂肪酶B（CAL-B），以4:1的N,N-二甲基甲酰胺/己烷混合物作为反应介质，对外消旋9-(2,3-二羟基丙基)腺嘌呤（DHPA，一种已获批准的抗病毒药物）进行酶促区域选择性单棕榈酰化反应。为提高所需单棕榈酰化反应的化学产率，对脂肪酶进行了固相化学修饰评估。在用新鲜的固定化化学糖基化CAL-B对产物溶液进行二次处理后，反应产率成功提高，获得了100%的产物。
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