摘要
((2S,4R)-4-Hydroxy-N-(2-methylnaphthalen-l-yl)pyrrolidine-2-carboxamide (HMNPC), an amide derived from 4-hydroxy-L-proline and 2-methyl naphthalen-l-amine, is a powerful ligand for Cu-catalyzed coupling of (het- ero)aryl halides with sulfinic acid salts, allowing for first time the metal-catalyzed coupling of (hetero)aryl chlorides and NaSO2Me. A considerable number of (hetero)aryl chlorides worked well, providing the pharmaceutically im- portant (hetero)aryl methylsulfones in good to excellent yields.
((2S,4R)-4-Hydroxy-N-(2-methylnaphthalen-l-yl)pyrrolidine-2-carboxamide (HMNPC), an amide derived from 4-hydroxy-L-proline and 2-methyl naphthalen-l-amine, is a powerful ligand for Cu-catalyzed coupling of (het- ero)aryl halides with sulfinic acid salts, allowing for first time the metal-catalyzed coupling of (hetero)aryl chlorides and NaSO2Me. A considerable number of (hetero)aryl chlorides worked well, providing the pharmaceutically im- portant (hetero)aryl methylsulfones in good to excellent yields.
基金
The authors are grateful to Chinese Academy of Sciences (supported by the Strategic Priority Research Program, grant XDB20020200 & QYZDJ-SSW- SLH029) and the National Natural Science Foundation of China (grant 21621002) for their financial support.