基于Buchwald-Hartwig反应合成N^6-芳氨基脱氧腺苷衍生物

Synthesis of N^6-Arylamino-2’-deoxyadenosine via Buchwald-Hartwig Reaction

N^6-芳氨基脱氧腺苷类化合物是一类重要的抗肿瘤药物分子,具有广泛的医疗价值.以2’-脱氧腺苷为原料,基于Buchwald-Hartwig反应,通过亚铜催化交叉偶联反应合成了一系列N^6-芳氨基脱氧腺苷衍生物(1a～1g),得到了一条高产率的N^6位修饰合成路线,为新型抗肿瘤药物合成提供参考.所得关键中间体及产物结构经IR,~1H NMR和^(13)C NMR得到确证.

N6-arylaminodeoxyadenosine is an important kind of antitumor drugs with wildly medical activity.Using 2’-deoxyadenosine as raw material,based on Buchwald-Hartwig reaction,a series of compounds (1a^1g) were synthesized by cuprous-catalyzed cross-coupling reaction.Intermediates and title compounds were confirmed by IR, 1H NMR and 13 C NMR.A high-yield N 6-modified synthetic route was obtained,which provides a reference for the synthesis of novel anti-tumor drugs.