An enzymatic glycosylation of nucleoside analogues using 尾-galactosidase from Escherichia coli

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• 作者：Ji艡í ; Bla啪ek^a ; ^b ; ^{blazek@uochb.cas.cz} ; Petr Jansa^a ; Ond艡ej Baszczy艌ski^a ; ^b ; Martin Maxmilian Kaiser^a ; Miroslav Otmar^a ; Marcela Kre膷merov&aacute ; ^a ; ^{marcela@uochb.cas.cz} ; Martin Dran膷í ; nský ; ^a ; Antoní ; n Holý ; ^a ; Blanka Kr&aacute ; lov&aacute ; ^b
• 关键词：Glycosylation ; Galactosylation ; 尾-Galactosidase ; Prodrug
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2012
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：1 May, 2012
• 卷：20
• 期：9
• 页码：3111-3118
• 文件大小：2096 K

摘要

A new enzymatic method for the synthesis of 尾-galactosides of nucleosides and acyclic nucleoside analogues has been developed, using 尾-galactosidase from Escherichia coli as a catalyst and lactose as a sugar donor. The method is very rapid, feasible and last but not least inexpensive. Its applicability has been proven for a broad variety of possible substrates with respect to its scaling up for preparative use. Five new compounds from a series of nucleoside and acyclic nucleoside analogues have been prepared on a scale of several hundred milligrams, in all cases revealing very good results of the method concerning the reproducibility of the reaction yields and simplicity of the purification process.