Summary of main observation and conclusion Owing to the easy functionalization of 3-haloindolines to many biologically active compounds,extensive efforts have been made for their efficient preparation.Herein,an electr...Summary of main observation and conclusion Owing to the easy functionalization of 3-haloindolines to many biologically active compounds,extensive efforts have been made for their efficient preparation.Herein,an electrochemical dearomative bromo-and chloro-cyclization of tryptamine and tryp-tophol derivatives has been developed under undivided electrolytic conditions.In this protocol,neither external chemical oxidants nor harsh conditions are needed,and a wide range of substituted hexahydropyrroloindolines/tetrahydrofuroindolines are obtained with halide ion in high efficiencies.Moreo-ver,this electrolysis could also be scaled up to gram synthesis with good yields.展开更多
Medium-sized nitrogen heterocycles are prevalent motifs in many kinds of bioactive molecules and natural products.Owing to the unfavorable enthalpic and entropic barriers during the transition states,access to medium-...Medium-sized nitrogen heterocycles are prevalent motifs in many kinds of bioactive molecules and natural products.Owing to the unfavorable enthalpic and entropic barriers during the transition states,access to medium-sized rings is challenging.Herein,a general and practical electrochemical ringexpansion protocol has been developed from commercially available benzocyclic ketones and amides.In this regard,a series of highly functionalized eightto eleven-membered lactams could be successfully accessed in high yields and efficiencies.展开更多
基金This work was supported by the National Natural Science Foundation of China(No.21520102003)the Hubei Province Natural Science Foundation of China(No,2017CFA010)The Pro-gram of Introducing Talents of Discipline to Universities of China(111 Program)is also appreciated.
文摘Summary of main observation and conclusion Owing to the easy functionalization of 3-haloindolines to many biologically active compounds,extensive efforts have been made for their efficient preparation.Herein,an electrochemical dearomative bromo-and chloro-cyclization of tryptamine and tryp-tophol derivatives has been developed under undivided electrolytic conditions.In this protocol,neither external chemical oxidants nor harsh conditions are needed,and a wide range of substituted hexahydropyrroloindolines/tetrahydrofuroindolines are obtained with halide ion in high efficiencies.Moreo-ver,this electrolysis could also be scaled up to gram synthesis with good yields.
基金the National Natural Science Foundation of China(no.21520102003)the Hubei Province Natural Science Foundation of China(no.2017CFA010)the Program of Introducing Talents of Discipline to Universities of China(111 Program)for their generous financial support.
文摘Medium-sized nitrogen heterocycles are prevalent motifs in many kinds of bioactive molecules and natural products.Owing to the unfavorable enthalpic and entropic barriers during the transition states,access to medium-sized rings is challenging.Herein,a general and practical electrochemical ringexpansion protocol has been developed from commercially available benzocyclic ketones and amides.In this regard,a series of highly functionalized eightto eleven-membered lactams could be successfully accessed in high yields and efficiencies.
