Studies On Synthesis Of Lamivudine And The Derivatives

Lamivudine is a HIV-RT inhibitor, at first used in treating HIV infection, later used asthe inhibitor of HBV duplication. The targets of lamivudine are HIV-RT andHBV-RDDP. Because lamivudine has many advantages, such as good tolerance, securityand convenience, it has been widely applied in clinic . The discovery of new drugs forHIV and HBV infection therapy ,and the current technology improvement of effectivedrugs have become the emphasis in current research, in the case of still lack of treatmentmethods for the both viral infectious diseases .This article summarized the epidemiologic study, prevention , treatment, antiviroticmedicine of nucleoside analogues , research condition of AIDS (acquired immunedeficiency syndrome) and HB (Hepatitis B). Based on literatures, a reasonable routineto synthesize lamivudine is selected. The reaction condition of each step is optimized sothat better quality and yield can be got.This technology has four steps in all, and the main intermediates can be synthesizedthrough esterification,condensations substitution,saccharide and reduction. The structureof each intermediate and the target molecular have been confirmed by melt point,massspectrum and proton-nuclear magnetic resonance .In the first step of this technology, we confirmed the appropriate ratio and the amount ofsulfate acid as catalyst.In the second step, we reduced the process of reflux, so the instrumenttation is simplified,and the maneuverability is enhanced, which is the high light of this technology. In thethird step, we changed the solvent system of chlorination and the silanization catalyst,so the purpose is more focused, and the energy consumption is lower. In the fourth step,we use hydroboration sodium as reducer, so the process is convenient, and the requestfor the solvent treatment is lower.This technology for preparation of lamivudine and its derivatives has many advantages,facile raw material, low equipment request, better feasibility, and high yield. So thistechnology has suitable industrial production prospect.