Enantioselective Organocatalytic Mannich Reaction and Fluorination Sequence of Pyrazolones to Isatin‐derived Ketimines

[摘要] An efficient asymmetric synthesis of oxindole‐pyrazolone adducts via organocatalytic Mannich reaction of 1‐phenyl‐1H‐pyrazol‐5(4H)‐ones with ketimine derivatives derived from isatins, followed by sequential electrophilic fluorination, has been developed. This approach offers a facile way to prepare chiral 3‐amino‐3‐(4‐fluoropyrazol‐4‐yl)‐substituted oxindole derivatives with a wide range of functional group tolerance.

[学科分类] 化学（综合）

[关键词] Oxindole‐pyrazolone adducts;Bifunctional organocatalyst;Ketimines;Pyrazolones