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
Azomethine ylides are useful intermediates for the rapid construction of chiral N-containing compounds.However,its synthetic potential has not been fully developed due to the limited reaction models.In combination wit...Azomethine ylides are useful intermediates for the rapid construction of chiral N-containing compounds.However,its synthetic potential has not been fully developed due to the limited reaction models.In combination with synergistic catalysis and azomethine ylide chemistry,we have developed several types of novel catalytic system including Cu/Pd,Cu/Ir and PTC/Ir catalysis;which can convert readily-available azomethine ylides to various high-valued molecules such as unnatural a-amino acids,homoallylic amines and N-heterocycles.Compared with the traditional mono-catalysis,the synergistic catalyst system exhibits enhanced catalytic efficiency and chiral induction ability in many cases.In addition,we have demonstrated that these strategies could be applied in the construction of bioactive compounds and natural products.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C.J.W.thanks the NSFC(Grants 21772147,21525207,21372180,21172176,20972117,20702039)for financial supportthe Program of Introducing Talents of Discipline to Universities of China(111 Project)is also appreciated.
文摘Azomethine ylides are useful intermediates for the rapid construction of chiral N-containing compounds.However,its synthetic potential has not been fully developed due to the limited reaction models.In combination with synergistic catalysis and azomethine ylide chemistry,we have developed several types of novel catalytic system including Cu/Pd,Cu/Ir and PTC/Ir catalysis;which can convert readily-available azomethine ylides to various high-valued molecules such as unnatural a-amino acids,homoallylic amines and N-heterocycles.Compared with the traditional mono-catalysis,the synergistic catalyst system exhibits enhanced catalytic efficiency and chiral induction ability in many cases.In addition,we have demonstrated that these strategies could be applied in the construction of bioactive compounds and natural products.
