The title compound 3 was synthesized from diethylguanidine nitrate（2） obtained from diethylamine, CaCN2 and HNO3. The mixture consisted of 0.5 mol 2, 0.55 mol acetonyl propionate, 3 g benzyltriethylammonium chloride...The title compound 3 was synthesized from diethylguanidine nitrate（2） obtained from diethylamine, CaCN2 and HNO3. The mixture consisted of 0.5 mol 2, 0.55 mol acetonyl propionate, 3 g benzyltriethylammonium chloride, and 44 g NaOH was refluxed for 4 hours to give 85 g 3, in yield 94.6%.展开更多
A compound ethyl(5S,6R)-2-(4-methylphenyl)-6-[(1R)-tert-butyldimethylsilyloxyethy]-penem-3-carboxylate was synthesized through displacement,acylation and Wittig cyclization reaction of optically active material(3R,4R)...A compound ethyl(5S,6R)-2-(4-methylphenyl)-6-[(1R)-tert-butyldimethylsilyloxyethy]-penem-3-carboxylate was synthesized through displacement,acylation and Wittig cyclization reaction of optically active material(3R,4R)-3-[(1R)-tert-butyldimethylsilyloxyethyl]-4-acetoxy-2-azetidi-none(4AA)upon thionocarboxlic acid.The intermediates and the target product were characterized by 1HNMR,IR,elementary analysis and MS.展开更多
Nucleoside reverse transcriptase inhibitors are the only drugs so far approved for the treatment of AIDS. Several nucleoside analogs are potent inhibitors of human immunodeficiency virus(HIV) in cell culture. However,...Nucleoside reverse transcriptase inhibitors are the only drugs so far approved for the treatment of AIDS. Several nucleoside analogs are potent inhibitors of human immunodeficiency virus(HIV) in cell culture. However, in many cases the nucleoside derivatives have a poor affinity for nucleoside kinases. Nucleoside 5′-phosphorothioates is relatively resistant to enzymatic transformations. In this paper, 2′,3′-O-alkoxymethylidene adenosine 5′-thiophosphoramidates were synthesized through a highly efficient approach. The new compounds were characterized by NMR, IR and ESI-MS.展开更多
文摘The title compound 3 was synthesized from diethylguanidine nitrate（2） obtained from diethylamine, CaCN2 and HNO3. The mixture consisted of 0.5 mol 2, 0.55 mol acetonyl propionate, 3 g benzyltriethylammonium chloride, and 44 g NaOH was refluxed for 4 hours to give 85 g 3, in yield 94.6%.
文摘A compound ethyl(5S,6R)-2-(4-methylphenyl)-6-[(1R)-tert-butyldimethylsilyloxyethy]-penem-3-carboxylate was synthesized through displacement,acylation and Wittig cyclization reaction of optically active material(3R,4R)-3-[(1R)-tert-butyldimethylsilyloxyethyl]-4-acetoxy-2-azetidi-none(4AA)upon thionocarboxlic acid.The intermediates and the target product were characterized by 1HNMR,IR,elementary analysis and MS.
文摘Nucleoside reverse transcriptase inhibitors are the only drugs so far approved for the treatment of AIDS. Several nucleoside analogs are potent inhibitors of human immunodeficiency virus(HIV) in cell culture. However, in many cases the nucleoside derivatives have a poor affinity for nucleoside kinases. Nucleoside 5′-phosphorothioates is relatively resistant to enzymatic transformations. In this paper, 2′,3′-O-alkoxymethylidene adenosine 5′-thiophosphoramidates were synthesized through a highly efficient approach. The new compounds were characterized by NMR, IR and ESI-MS.
