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研究了有机溶剂中酶促核苷类化合物3’-酯高区域选择性的合成反应,探讨了核苷结构中R1位取代基变化对酶促酰化反应的影响.结果表明:来源于Burkholderia cepacia的固定化脂肪酶PS IM在有机溶剂THF中的催化效果最佳,且酰化反应的优势位点均为3’-羟基(90%～>99%);随着核苷中R1位取代基由F变化至CF3或酰基供体链长由C6增加至C14,该酰化反应的3’-区域选择性均呈现逐渐增加的趋势,构效关系分析表明,这主要源于PS IM酶特殊的活性中心结构.
The high regioselectivity of the 3’-ester was investigated in organic solvents and the effect of the change of R1 substituent on the enzymatic acylation was investigated. The results showed that the 3’-ester from Burkholderia cepacia Of the immobilized lipase PS IM in organic solvents THF best catalytic effect, and the acylation reaction is the most favorable sites 3’-hydroxyl (90% ~> 99%); with the nucleoside R1 substituent The change from F to CF3 or the increase of the acyl donor chain length from C6 to C14 showed a tendency toward a gradual increase in the 3’-regioselectivity of the acylation reaction. The structure-activity relationship analysis indicated that this was mainly due to the special Active center structure.