【摘要】 研究1-烷基-5-氨基-6-苯乙基尿嘧啶（1a,1b）方便、高产率的合成方法,此类化合物有可能作为非核苷类HIV-1RT抑制剂。以6-甲基尿嘧啶（2）为起始物,经硝化、烷基化、苄基化及一锅反应脱苄基及还原反应等合成目标化合物,并用NMR、MS、IR、Anal鉴定化合物结构。探索出了一种合成1-烷基-5氨基-6-苯乙基尿嘧啶类化合物的方便方法。首次于用3或4步反应、高产率合成了1-烷基-5-氨基-6-苯乙基尿嘧啶（1a,1b）并发现化合物1a有中度抗HIV-1RT的活性(IC₅₀=29μM)。更多还原

【Abstract】 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 simulta- neously 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.更多还原