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
2-Acetamidoacrylic acid or methyl 2-acetamidoacrylate is reacted with solution of sodium of methylselenol to give N-acetyl-Se-methylselenocysteine.The L(and D)-Se-methylselenocysteine have been prepared in high optica...2-Acetamidoacrylic acid or methyl 2-acetamidoacrylate is reacted with solution of sodium of methylselenol to give N-acetyl-Se-methylselenocysteine.The L(and D)-Se-methylselenocysteine have been prepared in high optical purity by treating N-acetyl-Se-methylselenocysteine in water using acylase I from porcine kidney as a catalyst.The influencing factors on the resolution reaction are discussed by orthogonal experiment,including pH value,reaction temperature,concentration of Co2+ and amount of acylase I.Under the optimizing resolution conditions,L(and D)-Se-methylselenocysteine are obtained with>96 % optical purity in about 40% yield.展开更多
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.
文摘2-Acetamidoacrylic acid or methyl 2-acetamidoacrylate is reacted with solution of sodium of methylselenol to give N-acetyl-Se-methylselenocysteine.The L(and D)-Se-methylselenocysteine have been prepared in high optical purity by treating N-acetyl-Se-methylselenocysteine in water using acylase I from porcine kidney as a catalyst.The influencing factors on the resolution reaction are discussed by orthogonal experiment,including pH value,reaction temperature,concentration of Co2+ and amount of acylase I.Under the optimizing resolution conditions,L(and D)-Se-methylselenocysteine are obtained with>96 % optical purity in about 40% yield.
