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
The selective epoxidation of 3,3-(1,2-ethanediyl-bisoxy)-5(10),9(11)-estradiene-17-α-(1-propynyl)-17-β-ol with Fe(Ⅱ)Pc/PhIO was investigated at 25 ℃? atmospheric pressure. With a molar ratio of Fe(Ⅱ)Pc∶compound...The selective epoxidation of 3,3-(1,2-ethanediyl-bisoxy)-5(10),9(11)-estradiene-17-α-(1-propynyl)-17-β-ol with Fe(Ⅱ)Pc/PhIO was investigated at 25 ℃? atmospheric pressure. With a molar ratio of Fe(Ⅱ)Pc∶compound(I)∶PhIO at 6.25∶50∶120, the conversion reaches 100%. The overall yield of the products 5α, 10α-epoxide(2) and 5β, 10β-epoxide(3)is 60%, and the molar ratio of 2 to 3 is {8.39∶}1. The product 5α, 10α-epoxide is identified by melting point and HPLC.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The selective epoxidation of 3,3-(1,2-ethanediyl-bisoxy)-5(10),9(11)-estradiene-17-α-(1-propynyl)-17-β-ol with Fe(Ⅱ)Pc/PhIO was investigated at 25 ℃? atmospheric pressure. With a molar ratio of Fe(Ⅱ)Pc∶compound(I)∶PhIO at 6.25∶50∶120, the conversion reaches 100%. The overall yield of the products 5α, 10α-epoxide(2) and 5β, 10β-epoxide(3)is 60%, and the molar ratio of 2 to 3 is {8.39∶}1. The product 5α, 10α-epoxide is identified by melting point and HPLC.
