Fluorocyclization of Vinyl Azides for the Formation of 3-Azido Heterocycles.

Diangang BaiLinxuan LiXiaomeng LiYing LuYong WuBhoomireddy Rajendra Prasad ReddYongquan Ning
Published in: Chemistry, an Asian journal (2020)
3-Azido saturated heterocycles are important for therapeutic-development but challenging to prepare. Disclosed herein is a novel synthetic strategy for 3-azido heterocycles via fluorocyclization of the easily available vinyl azides. This transfor-mation proceeded under mild conditions and provided a wide range of 3-azido heterocycles in good to excellent yields. Notably, the azido group plays an indispensable role to promote rapid and regioselective fluorocyclization. Moreover, the protocol was highlighted by gram-scale synthesis and further synthetic transformations.