Aza-Henry/Hemiketamination Tandem Reactions of N-(Benzothiazol-2-yl)imines and 4-nitro-1-phenylbutan-1-one
There being relatively little study on C2 synthons with N-(benzothiazol-2-yl)imines in recent years,the new method study is important for C2 synthons to generate a series of heterocyclic derivatives based on N-(ben-zothiazol-2-yl)imines.In this paper,a series of N-(hetero)arylpiperidine molecules containing benzothiazole scaf-folds were successfully designed and synthesized based on aza-Henry/hemiketamination tandem reaction.An ef-fective method was constructed for synthesizing N-(hetero)arylpiperidine molecules making use of N-(ben-zothiazol-2-yl)imines and 4-nitro-l-phenylbutan-l-one as the reaction substrates,dichloromethane as the solvent,and potassium phosphate trihydrate(10％mol)as the catalyst at room temperature.Results show that a series of desired products can be obtained in high yield with moderate stereoselectivity,and the tandem reaction still can maintain a better yield and stereoselectivity at the gram-scale.
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维普
