Enzymatic Synthesis of 5-O-acylcytarabine Vinyl Ester and Preparation of Polymeric Prodrugs of Cytarabine

摘要：

We developed a facile protocol of regioselective enzymatic acylation of primary hydroxyl group of cytarabine using divinyl dicarboxylates as acyl donor. Polymerizable 5-Oacylcytarabine derivatives (2a～2d) were synthesized by immobilized lipase Novozym 435 from Candida Antarctica type B in anhydrous acetone in high yield and excellent regioselectivity. These resulting monomers were subject to the further polymerization in the second step. Homopolyrnerization in DMF with AIBN as initiator gave polymeric prodrugs (3a～3d). The obtained polymeric prodrugs were characterized with IR and NMR.

关键词： enzymatic synthesis cytarabine regioselective homopolymer

作者: WANG Ya-juan QUAN Jing WU Jin-xian Yu Yang ZHU Li-min

作者单位: College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, Shanghai, 201620, College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, Shanghai, 201620,

会议类型: 国际会议

会议名称: 2010 International Forum on Biomedical Textile Materials(2010国际纺织生物医用论坛)

会议地点: 上海

会议语种:英文

页码: 135-140

在线出版日期: 2010-05-28（万方平台首次上网日期，不代表论文的发表时间）