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Herein, a B(C6F5)3-catalyzed formal (n + 3) (n = 5 and 6) cycloaddition of bicyclo1.1.0butanes (BCBs) with imidazolidines/hexahydropyrimidines is described. The reaction provides a modular, atom-economical, and efficient strategy to two libraries of synthetically challenging medium-bridged rings, 2,5-diazabicyclo5.1.1nonanes and 2,6-diazabicyclo6.1.1decanes, in moderate to excellent yields. This reaction also features simple operation, mild reaction conditions, and broad substrate scope. A scale-up experiment and various synthetic transformations of products further highlight the synthetic utility.
Yang et al. (Fri,) studied this question.
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