1-Alkyl-5-amino-6-phenylethyluracils （1a, 1b） were synthesized as potential non-nucleoside HIV-1RT inhibitors. A convenient synthetic procedure was developed for the preparation of 1-alkyl-5-amino or 5-aminosubstitu...1-Alkyl-5-amino-6-phenylethyluracils （1a, 1b） were synthesized as potential non-nucleoside HIV-1RT inhibitors. A convenient synthetic procedure was developed for the preparation of 1-alkyl-5-amino or 5-aminosubstituted-6-phenylethyluracils, which were synthesized in three or four steps from 6-methyluracil in good yield. The development of a one-pot reaction that simultaneously removed the benzyl protection group and reduced the nitro group greatly improved the yield of the synthesis. Compounds 1a and 1b are analogs of MKC-442, which is an efficient inhibitor of HIV-1 reverse transcriptase, 1a and 1b were tested for their inhibition of HIV-1RT, and moderate activity was found for 1a.展开更多
2α,3α-epoxy-16β-(1-pyrrolidinyl)-androstan-17β-ol,a main intermediate of Rocuronium bromide,was synthesized from epiandrosterone by elimination,bromination,epoxidation,N-alkylation and reduction with assisted micr...2α,3α-epoxy-16β-(1-pyrrolidinyl)-androstan-17β-ol,a main intermediate of Rocuronium bromide,was synthesized from epiandrosterone by elimination,bromination,epoxidation,N-alkylation and reduction with assisted microwave irradiation.The new approach could significantly shorten the reaction time,improve the reaction selectivity and the yield.The structures were confirmed by 1H-NMR and MS.展开更多
基金National Science Foundation of China (Grant No.20672)the Doctoral grant of the Ministry of Education of China(Grant No.2007000174).
文摘1-Alkyl-5-amino-6-phenylethyluracils （1a, 1b） were synthesized as potential non-nucleoside HIV-1RT inhibitors. A convenient synthetic procedure was developed for the preparation of 1-alkyl-5-amino or 5-aminosubstituted-6-phenylethyluracils, which were synthesized in three or four steps from 6-methyluracil in good yield. The development of a one-pot reaction that simultaneously removed the benzyl protection group and reduced the nitro group greatly improved the yield of the synthesis. Compounds 1a and 1b are analogs of MKC-442, which is an efficient inhibitor of HIV-1 reverse transcriptase, 1a and 1b were tested for their inhibition of HIV-1RT, and moderate activity was found for 1a.
文摘2α,3α-epoxy-16β-(1-pyrrolidinyl)-androstan-17β-ol,a main intermediate of Rocuronium bromide,was synthesized from epiandrosterone by elimination,bromination,epoxidation,N-alkylation and reduction with assisted microwave irradiation.The new approach could significantly shorten the reaction time,improve the reaction selectivity and the yield.The structures were confirmed by 1H-NMR and MS.
