A convenient synthesis of cis-（±） isomer 1 and trans-（±） isomer 2 of lamivudine starting from benzoyloxyacetaldehyde and 1,4-dithiane-2,5-diol is described. The key steps include chlorination of oxathiol...A convenient synthesis of cis-（±） isomer 1 and trans-（±） isomer 2 of lamivudine starting from benzoyloxyacetaldehyde and 1,4-dithiane-2,5-diol is described. The key steps include chlorination of oxathiolane lactol 5 by SOCl2/DMF, followed by coupling with silylated N^4- acetylcytosine and deprotection. The overall yield was 42.6 % and 20,1%, respectively.展开更多
文摘A convenient synthesis of cis-（±） isomer 1 and trans-（±） isomer 2 of lamivudine starting from benzoyloxyacetaldehyde and 1,4-dithiane-2,5-diol is described. The key steps include chlorination of oxathiolane lactol 5 by SOCl2/DMF, followed by coupling with silylated N^4- acetylcytosine and deprotection. The overall yield was 42.6 % and 20,1%, respectively.
