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偕二氟炔丙基取代的芳烃是一类非常重要的化合物,但传统合成该类化合物的方法却存在很大局限性.以过渡金属催化直接向芳烃偕二氟炔丙基化是一种高效简洁制备上述化合物的方法.以廉价易得的Ni(NO3)2?6H2O为催化剂,首次实现了镍催化下芳基硼酸与α,α-二氟炔丙基溴的偶联反应.该反应不仅温和高效、原料廉价易得、官能团兼容性良好,而且还能进行克量级放大和对生物活性分子的后期氟修饰,从而为新药研发提供了一种有效手段.
Gemination of difluoropropargyl-substituted aromatics is a very important class of compounds, but the traditional methods for the synthesis of these compounds are very limited. The transition metal catalyzed directly to the aryldifluoro propargylated aromatic is a highly efficient A simple and convenient method for the preparation of the above compounds was proposed.The nickel-catalyzed coupling reaction of arylboronic acid with α, α-difluoropropargyl bromide was firstly achieved with cheap and readily available Ni (NO3) 2 · 6H2O as catalyst. Mild and efficient, cheap and easy to get raw materials, good functional group compatibility, but also for gram-level amplification and post-fluoro modification of bioactive molecules, thus providing an effective means for the development of new drugs.