Facile One-pot Protocol of Derivatization Nitropyridines: Access to 3-Acetamidopyridin-2-yl 4-methylbenzenesulfonate Derivatives

[摘要] This paper discloses an efficient one-pot protocol to convert easily accessible 3-nitropyridines to 3-acetamidopyridin-2-yl 4-methylbenzenesulfonate derivatives which are core structures of many pharmaceutical molecules. The strategy successfully combined a three-step reaction in one pot via progressively adding different reactants at rt. The reaction displays good functional group tolerance and regioselectivity. Structurally diversified 3-nitropyridine could be time-efficiently (3.5 h) derivatized to various functional 2- O ,3- N -pyridines which are apt for further elaborations. The transformation was amenable to gram-scale synthesis.

[学科分类] 内科医学

[关键词] One-pot;[3;3]-sigmatropic rearrangement;heteroarene;pyridine derivatives;late-stage functionalization