Abstract

Abstract: The construction of bicyclo[1.1.1.]pentanes (BCPs) typically require the cumbersome use of labile [1.1.1.]propellane in solution and involve multicomponent radical reactions, which commonly produce undesired by‐products that hinder the efficient construction of BCPs. In this paper, we present a catalyst‐free strategy by constructing an electron donor‐acceptor (EDA) complex utilizing the naturally electron‐deficient nature of BCP thianthrenium salt, which were irradiated with visible light to obtain trifluoromethyl‐BCP radicals through a SET process, subsequently reacted with various substituted quinoxalines. Moreover, the successful structural modification of drug molecule derivatives confirm the utility of this scheme in the field of drug discovery.

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