环加成
化学
烯烃
吡唑啉
分子间力
三氮烯
路易斯酸
催化作用
组合化学
有机催化
有机化学
立体化学
对映选择合成
分子
作者
Shiyong Peng,Huihui Zhu,Haiyun Wu,Dejun Hao,Liangliang Yang,Yangyang Liu,Xue Gong,Jianhe Wei,Lei Wang
标识
DOI:10.1002/chem.202300562
摘要
Abstract A novel approach to chemoselective synthesis of biologically important CF 3 ‐subsituted pyrazolines was developed via a Lewis base catalyzed intermolecular triazene cycloaddition reaction of an array of terminal/internal alkenes with CF 3 CHN 2 . This strategy features a catalytic amount of 1,8‐diazabicyclo[5.4.0]undec‐7‐ene, high yields (up to 95 %), wide substrate scope and excellent functional group tolerance (54 examples). Importantly, we preformed scaffold diversification of a panel of known pharmaceuticals, natural products, and bioactive heterocycles to generate the corresponding pyrazoline derivatives with potential broad bioactivities for further development.
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