Heterocycle-braced cyclic peptides have demonstrated enhanced metabolic stability,increased potency and selectivity.Here,we present a rapid synthesis method for constructing Trp(C7)-alkene(E)-crosslinked cyclic peptid...Heterocycle-braced cyclic peptides have demonstrated enhanced metabolic stability,increased potency and selectivity.Here,we present a rapid synthesis method for constructing Trp(C7)-alkene(E)-crosslinked cyclic peptides with potent anti-proliferative activities against cancer cells,through C-H alkenylation and macrolactamization.This report addresses critical challenges associated with the installation and removal of the directing group N-Piv,configuration selectivity of the olefin,and intramolecular cyclization.No-tably,this method exhibits mild reaction conditions,traceless removal of the directing group,and high configuration selectivity.展开更多
Cp^*Co(Ⅲ)-catalyzed direct C—H amidation of azines has been developed.This co nversion could proceed smoothly in the absence of external oxidants,acids or bases,with excellent regioselectivity and broad functional g...Cp^*Co(Ⅲ)-catalyzed direct C—H amidation of azines has been developed.This co nversion could proceed smoothly in the absence of external oxidants,acids or bases,with excellent regioselectivity and broad functional group tolerance,CO2 was released as the sole byproduct,thus providing an environmentally benign amidation process.The products obtained are important intermediates in organic synthesis.展开更多
Rhodium(Ⅲ)-catalyzed[4+1]cyclization of azobenzenes with α-Cl ketones has been developed.3-Acyl-2H-indazoles could be easily afforded in up to 97%yields for more than 30 examples.The obtained products are potentiall...Rhodium(Ⅲ)-catalyzed[4+1]cyclization of azobenzenes with α-Cl ketones has been developed.3-Acyl-2H-indazoles could be easily afforded in up to 97%yields for more than 30 examples.The obtained products are potentially valuable in organic synthesis and drug discovery.This protocol featured with high efficiency,extensive functional group tolerance and mild reaction conditions.The one-step efficient construction of an anti-inflammatory agent confirms the practicability of this procedure.展开更多
基金the National Key R&D Program of China(No.2022YFA1302900 to H.Liu)National Natural Science Foundation of China(Nos.82130105,22337003,82121005 to H.Liu+2 种基金and Nos.22177124,82322063 to J.Wang)Program of Shang-hai Academic Research Leader(No.23XD1460300 to J.Wang)the Lingang Laboratory(No.LG-GG-202204-02 to J.Wang)for supporting this work.We would like to acknowledge Shanghai Highline Therapeutics.
文摘Heterocycle-braced cyclic peptides have demonstrated enhanced metabolic stability,increased potency and selectivity.Here,we present a rapid synthesis method for constructing Trp(C7)-alkene(E)-crosslinked cyclic peptides with potent anti-proliferative activities against cancer cells,through C-H alkenylation and macrolactamization.This report addresses critical challenges associated with the installation and removal of the directing group N-Piv,configuration selectivity of the olefin,and intramolecular cyclization.No-tably,this method exhibits mild reaction conditions,traceless removal of the directing group,and high configuration selectivity.
基金the Ministry of Science and Technology of China(No.2016YFE0132600)Henan Center for Outstanding Overseas Scientists(No.GZS2020001)。
文摘Cp^*Co(Ⅲ)-catalyzed direct C—H amidation of azines has been developed.This co nversion could proceed smoothly in the absence of external oxidants,acids or bases,with excellent regioselectivity and broad functional group tolerance,CO2 was released as the sole byproduct,thus providing an environmentally benign amidation process.The products obtained are important intermediates in organic synthesis.
基金This work was supported by the National Natural Science Foundation of China(No.21572072)111 Project(No.BC 2018061)Xiamen Southern Oceanographic Center(No.15PYY052SF01).
文摘Rhodium(Ⅲ)-catalyzed[4+1]cyclization of azobenzenes with α-Cl ketones has been developed.3-Acyl-2H-indazoles could be easily afforded in up to 97%yields for more than 30 examples.The obtained products are potentially valuable in organic synthesis and drug discovery.This protocol featured with high efficiency,extensive functional group tolerance and mild reaction conditions.The one-step efficient construction of an anti-inflammatory agent confirms the practicability of this procedure.
