B(C6F5)3-Catalyzed [2π + 2σ] Cycloadditions of Carbodiimides with Bicyclo[1.1.0]butanes
Lei Xiao1, Lin Li1, Yishan Xiong1
1Institute of Drug Discovery Technology and Qian Xuesen Collaborative Research Center of Astrochemistry and Space Life Sciences, Ningbo University, Ningbo 315211, Zhejiang China.
Abstract:
Amidines are a privileged structural motif in a series of pharmaceuticals. In this work, we developed a simple, scalable, and transition-metal-free method for the efficient [2π + 2σ] cycloaddition of carbodiimides with bicyclo[1.1.0]butanes. The approach enabled the synthesis of 28 examples of functionalized amidines under mild reaction conditions in up to 99% yield with Z/E ratios of up to >19:1.
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