CAJ | 학술논문

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-锅反应脱苄基及还原反戍等合成目标化合物,并用NMR、MS、IR、Anal签定化合物结构.探索出了一种合成1-烷基-5氨基-6-苯乙基尿啼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=29 μM).
연구1-완기-5-안기-6-분을기뇨밀정(1a,1b)방편、고산솔적합성방법,차류화합물유가능작위비핵감류HIV-1RT억제제.이6-갑기뇨밀정(2)위기시물,경초화、완기화、변기화급-과반응탈변기급환원반수등합성목표화합물,병용NMR、MS、IR、Anal첨정화합물결구.탐색출료일충합성1-완기-5안기-6-분을기뇨제정류화합물적방편방법.수차우용3혹4보반응、고산솔합성료1-완기-5-안기-6-분을기뇨밀정(1a,1b)병발현화합물1a유중도항HIV-1RT적활성(IC50=29 μM).
1-Alkyl-5-amino-6-phenylethyluraeils (1a,1b) were synthesized as potential non-nueleoside HIV-1 RT inhibitors.A convenient synthetic procedure was developed for the preparation of l-alkyl-5-amino or 5-aminosubstituted-6-phenylethyluraeils,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.