We present herein an unconventional tandem [3,3]-sigmatropic rearrangement/[2+2] cycloaddition of simple dipropargylphosphonates to deliver a range of bicyclic polysubstituted cyclobutenes and cyclobutanes under Ag/Co relay catalysis. An interesting switch from allene-allene to allene-alkyne cycloaddition was observed based on the substitution of the substrates, which further diversified the range of compounds accessible from this practical method. Significantly, preliminary biological screening of these new compounds identified promising candidates as suppressor of cellular proliferation.

中文翻译：

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Ag/Co 中继催化下二炔丙基膦酸酯串联 [3,3]-Sigmatropic 重排/[2+2] 环加成反应获得取代环丁烯


我们在此提出了简单的二炔丙膦酸酯的非常规串联[3,3]-σ重排/[2+2]环加成，以在Ag/Co中继催化下产生一系列双环多取代环丁烯和环丁烷。基于底物的取代，观察到从丙二烯-丙二烯到丙二烯-炔环加成的有趣转变，这进一步使该实用方法可获得的化合物范围多样化。值得注意的是，对这些新化合物的初步生物筛选确定了有希望作为细胞增殖抑制剂的候选化合物。