A novel series of pyrrolidinone analogs that are designed as Michael addition acceptors to react irreversibly with the proteasome active site Thr1O~γhave been synthesized.Although biological evaluation results show t...A novel series of pyrrolidinone analogs that are designed as Michael addition acceptors to react irreversibly with the proteasome active site Thr1O~γhave been synthesized.Although biological evaluation results show that the compounds display poor inhibitory activity towards the proteasome active sites,pyrrolidinone analogs might still be modified to be potential 20S proteasome inhibitors.展开更多
An efficient procedure for the selective preparation of hydroxy-,carbonyl-and acetal-containing 2-pyrrolidinones has been developed through radical cyclization of 1,6-dienes initiated byα-C(sp3)-H functionalization o...An efficient procedure for the selective preparation of hydroxy-,carbonyl-and acetal-containing 2-pyrrolidinones has been developed through radical cyclization of 1,6-dienes initiated byα-C(sp3)-H functionalization of alcohols.This protocol could be conducted at catalyst-free conditions at relatively low temperature(80℃)by employing commercially available tert-butyl peroxybenzoate(TBPB)as the oxidant.展开更多
Asymmetric synthesis of novel optically active nucleoside analogues 7 from natural tartaric acid is described. In the given nucleoside analogues an optically active polyhydroxy pyrrolidinonyl ring is in place of the t...Asymmetric synthesis of novel optically active nucleoside analogues 7 from natural tartaric acid is described. In the given nucleoside analogues an optically active polyhydroxy pyrrolidinonyl ring is in place of the tetrahydrofuran ring.展开更多
文摘A novel series of pyrrolidinone analogs that are designed as Michael addition acceptors to react irreversibly with the proteasome active site Thr1O~γhave been synthesized.Although biological evaluation results show that the compounds display poor inhibitory activity towards the proteasome active sites,pyrrolidinone analogs might still be modified to be potential 20S proteasome inhibitors.
基金the National Natural Science Foundation of China(No.21801142)the Natural Science Foundation of Zhejiang Province(No.LQ18B020002)+1 种基金the Ningbo Municipal Natural Science Foundation(No.2019A610021)the Hunan Provincial NaturalScience Foundation of China(No.2019JJ20008)for financial support。
文摘An efficient procedure for the selective preparation of hydroxy-,carbonyl-and acetal-containing 2-pyrrolidinones has been developed through radical cyclization of 1,6-dienes initiated byα-C(sp3)-H functionalization of alcohols.This protocol could be conducted at catalyst-free conditions at relatively low temperature(80℃)by employing commercially available tert-butyl peroxybenzoate(TBPB)as the oxidant.
文摘Asymmetric synthesis of novel optically active nucleoside analogues 7 from natural tartaric acid is described. In the given nucleoside analogues an optically active polyhydroxy pyrrolidinonyl ring is in place of the tetrahydrofuran ring.
