Hainan Branch of the Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences &, Peking Union Medical College, Haikou, Hainan, 570311, China.
School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, 529020, China.
Chemistry. 2023 Jul 14;29(40):e202300562. doi: 10.1002/chem.202300562. Epub 2023 May 31.
A novel approach to chemoselective synthesis of biologically important CF -subsituted pyrazolines was developed via a Lewis base catalyzed intermolecular triazene cycloaddition reaction of an array of terminal/internal alkenes with CF CHN . 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.
一种通过路易斯碱催化的一系列末端/内部烯烃与 CF CHN 的三氮烯环加成反应，来实现对生物重要的 CF -取代吡唑啉的化学选择性合成的新方法被开发出来。该策略的特点是使用催化量的 1,8-二氮杂双环[5.4.0]十一-7-烯，高收率（高达 95%），广泛的底物范围和出色的官能团耐受性（54 个例子）。重要的是，我们对一系列已知药物、天然产物和生物活性杂环进行了支架多样化，以生成具有潜在广泛生物活性的相应吡唑啉衍生物，用于进一步开发。
