Borylative cyclization of E-3-arylallyl carbamoyl chlorides is achieved through copper catalyzed intramolecular carboboration with B_(2)pin_(2).2-Aryl-3-boryl-γ-lactams are formed with exclusive cisdiastereoselectivi...Borylative cyclization of E-3-arylallyl carbamoyl chlorides is achieved through copper catalyzed intramolecular carboboration with B_(2)pin_(2).2-Aryl-3-boryl-γ-lactams are formed with exclusive cisdiastereoselectivity.CuBr-Dppp combination gives the best outcomes.The substrate scope is profiled.展开更多
When treated with an alkoxide base like t-BuOK in aprotic solvent,N-di phenyl methyl imino oxindoles,made conveniently through condensation of corresponding isatins with N-di phenyl methyl amine,are deprotonated to fo...When treated with an alkoxide base like t-BuOK in aprotic solvent,N-di phenyl methyl imino oxindoles,made conveniently through condensation of corresponding isatins with N-di phenyl methyl amine,are deprotonated to form azaallyl anions.Allylation and alkylation of this type of intermediates proceed smoothly with diverse C-electrophiles.Acidic work up finishes 3-amino-3-allyl/alkyl oxindoles.The overall transformation equals to an umpolung process at the C3 of isatins.展开更多
Inspired by the indolopyridoquinazoline scaffold of natural products evodiamine and rutaecarpine, novel triple G4 and Top1/2 ligands were rationally designed and synthesized. Systematic structure–activity relationshi...Inspired by the indolopyridoquinazoline scaffold of natural products evodiamine and rutaecarpine, novel triple G4 and Top1/2 ligands were rationally designed and synthesized. Systematic structure–activity relationship(SAR) studies led to the discovery of compound 15g, which effectively induced and stabilized G4 and inhibited Top1/2 with potent antitumor activity. Compound 15g represents a valuable chemical tool or lead compound for antitumor drug discovery. This proof-of-concept study also validated the feasibility of using planar natural products scaffold as templates to design new G4 ligands.展开更多
A ruthenium based catalytic system([Ru(p-cymene)Cl2]2/XantPhos with substoichiometric Cs2CO3)has been established to effectively achieve the first direct amination cyclization of 1,2,4-butanetriol with primary aromati...A ruthenium based catalytic system([Ru(p-cymene)Cl2]2/XantPhos with substoichiometric Cs2CO3)has been established to effectively achieve the first direct amination cyclization of 1,2,4-butanetriol with primary aromatic amines.The product of this sustainable hydrogen autotransfer process is valuable Naryl-3-pyrrolidinol.展开更多
A simple and nontoxic fluorescent chemosensor of di-O-methyl curcumin has been prepared from curcumin. The sensor exhibited selective and sensitive fluorescent responses toward A13＋ over a wide range of metal ions, s...A simple and nontoxic fluorescent chemosensor of di-O-methyl curcumin has been prepared from curcumin. The sensor exhibited selective and sensitive fluorescent responses toward A13＋ over a wide range of metal ions, such as Mn2＋, Ce3＋, Pt2＋, Sn4＋, Hg＋, Sb3＋, K＋, Ca2＋, Mg2＋, Ba2＋, Cu2＋＇ Ni2＋＇ Na＋＇ NH4＋＇ Ag＋＇ Pb2＋＇ Zn2＋＇ Fee＋＇ Fe3＋, Hg2＋ and Cr3＋ in ethanol/water. The free ligand showed quite weak fluorescence emission due to the isom- erization of C=O double bond in the excited state, however, after addition of Al3＋, fluorescence emission results in a prominent fluorescence enhancement.展开更多
基金the National Natural Science Foundation of China(No.21672027)for financial supportsupported by High-Level Entrepreneurial Talent Team of Jiangsu Province(No.2017-37)。
文摘Borylative cyclization of E-3-arylallyl carbamoyl chlorides is achieved through copper catalyzed intramolecular carboboration with B_(2)pin_(2).2-Aryl-3-boryl-γ-lactams are formed with exclusive cisdiastereoselectivity.CuBr-Dppp combination gives the best outcomes.The substrate scope is profiled.
基金the National Natural Science Foundation of China(No.21672027)for financial supportsupported by High-Level Entrepreneurial Talent Team of Jiangsu Province(No.2017-37)。
文摘When treated with an alkoxide base like t-BuOK in aprotic solvent,N-di phenyl methyl imino oxindoles,made conveniently through condensation of corresponding isatins with N-di phenyl methyl amine,are deprotonated to form azaallyl anions.Allylation and alkylation of this type of intermediates proceed smoothly with diverse C-electrophiles.Acidic work up finishes 3-amino-3-allyl/alkyl oxindoles.The overall transformation equals to an umpolung process at the C3 of isatins.
基金supported by the National Natural Science Foundation of China (Nos. 22077138 to S. Wu, 81725020 to C. Sheng81872742 to G. Dong)+1 种基金the National Key Research and Development Program of China (No. 2020YFA0509200 to C. Sheng)Shanghai Rising-Star Program (No. 22QA1411300 to S. Wu)。
文摘Inspired by the indolopyridoquinazoline scaffold of natural products evodiamine and rutaecarpine, novel triple G4 and Top1/2 ligands were rationally designed and synthesized. Systematic structure–activity relationship(SAR) studies led to the discovery of compound 15g, which effectively induced and stabilized G4 and inhibited Top1/2 with potent antitumor activity. Compound 15g represents a valuable chemical tool or lead compound for antitumor drug discovery. This proof-of-concept study also validated the feasibility of using planar natural products scaffold as templates to design new G4 ligands.
基金the National Natural Science Foundation of China (No. 21672027)QingLan Project of Jiangsu Province (2016)+1 种基金SixTalent-Peaks Program of Jiangsu (2016) for financial supportsupported by High-Level Entrepreneurial Talent Team of Jiangsu Province (No.2017-37)
文摘A ruthenium based catalytic system([Ru(p-cymene)Cl2]2/XantPhos with substoichiometric Cs2CO3)has been established to effectively achieve the first direct amination cyclization of 1,2,4-butanetriol with primary aromatic amines.The product of this sustainable hydrogen autotransfer process is valuable Naryl-3-pyrrolidinol.
基金the National Natural Science Foundation of China （Nos. 21002009 and 21572026）, the Scientific and Technological Project of Jiangsu Province （No. BY2014037-01）, the Natural Science Foundation of Jiangsu Colleges and Universities （No. 14KJA150002）, Qing Lan Project of Jiangsu Province, the Priority Academic Program Development （PAPD） of Jiangsu Higher Education Institutions, and the Jiangsu Key Laboratory of Advanced Catalytic Ma- terials and Technology （No. BM2012110）.
文摘A simple and nontoxic fluorescent chemosensor of di-O-methyl curcumin has been prepared from curcumin. The sensor exhibited selective and sensitive fluorescent responses toward A13＋ over a wide range of metal ions, such as Mn2＋, Ce3＋, Pt2＋, Sn4＋, Hg＋, Sb3＋, K＋, Ca2＋, Mg2＋, Ba2＋, Cu2＋＇ Ni2＋＇ Na＋＇ NH4＋＇ Ag＋＇ Pb2＋＇ Zn2＋＇ Fee＋＇ Fe3＋, Hg2＋ and Cr3＋ in ethanol/water. The free ligand showed quite weak fluorescence emission due to the isom- erization of C=O double bond in the excited state, however, after addition of Al3＋, fluorescence emission results in a prominent fluorescence enhancement.
