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目的对新型抗乙肝药物阿米福韦进行结构改造,设计合成新的前药。方法以2-氯乙醇为原料,经氯甲基化、取代、缩合、烃化、水解、缩合得到目标产物。结果合成了11个新结构化合物,并经1H-NMR、13C-NMR、MS确证结构。体外抗乙肝病毒活性测试结果显示,阿米福韦异丙基碳酸酯的抗病毒活性显著提高,为阿米福韦的100倍。结论阿米福韦碳酸酯能够更好的释放活性药物,提高抗病毒活性。
OBJECTIVE To construct the new anti-hepatitis B drug amifovir and to design and synthesize new prodrugs. Methods Starting from 2-chloroethanol, the target product was obtained by chloromethylation, substitution, condensation, alkylation, hydrolysis and condensation. Results Eleven new structural compounds were synthesized and confirmed by 1H-NMR, 13C-NMR and MS. In vitro anti-hepatitis B virus activity test results showed that the antiviral activity of amifovir isoproxyl carbonate significantly increased, 100 times that of the amifovir. Conclusions Ampicivoxil can release active drug better and increase antiviral activity.