Two novel monophosphoramidites were synthesized through a five-step transformation from commercially available L-proline. In the Rh-catalyzed asymmetric hydrogenation of α-dehydroamino acid derivatives, ligand （Sc,...Two novel monophosphoramidites were synthesized through a five-step transformation from commercially available L-proline. In the Rh-catalyzed asymmetric hydrogenation of α-dehydroamino acid derivatives, ligand （Sc,Rα）-1b showed good enantioselectivity and up to 91% e.e. was obtained.展开更多
Two new C2-symmetrical bidentate phosphoramidite ligands were synthesized and employed in the Rh-catalyzed asymmetric hydrogenation of β-（acylamino）acrylates, up to 89% ee with full conversions was obtained.
A new strategy is developed for the synthesis of 1-aminoisoquinoline derivatives.This Rh(III)-catalyzed[4+2]annulation reaction employs benzamidines as efficient directing groups and the vinylene carbonate as an acety...A new strategy is developed for the synthesis of 1-aminoisoquinoline derivatives.This Rh(III)-catalyzed[4+2]annulation reaction employs benzamidines as efficient directing groups and the vinylene carbonate as an acetylene surrogate.Additionally,the reaction features broad substrate scopes and good yields,only producing carbonate anion as byproduct.展开更多
The development of innovative strategies and methods to provide natural product-like macrocycles not accessible by biosynthesis, but endowed with novel bioactivities and simplified structure, is highly desirable. Insp...The development of innovative strategies and methods to provide natural product-like macrocycles not accessible by biosynthesis, but endowed with novel bioactivities and simplified structure, is highly desirable. Inspired by the key scaffolds of rapamycin and FR252921, herein, we report a Rh(III)-catalyzed C–H alkylation macrocyclization, which enables access to CF_(3)-substituted macrolides. DFT calculations reveal that the chemoselectivity between C–H alkylation and olefination macrocyclization was highly controllable. Moreover, the unique CF_(3)-substituted macrolides showed potent anti-inflammation activities against TNF-α, IL-6 and CCL2 m RNA expression.展开更多
A facile and efficient route to 4-aryl-2-[2-（trifluoromethylthio） aryl]quinazoline derivatives through a tandem directed Rh-catalyzed C-H iodination and trifluoromethylthiolation is described. The reaction proceeded...A facile and efficient route to 4-aryl-2-[2-（trifluoromethylthio） aryl]quinazoline derivatives through a tandem directed Rh-catalyzed C-H iodination and trifluoromethylthiolation is described. The reaction proceeded under mild reaction conditions, exhibited good functional group tolerance with a broad scope of substrate and excellent regi- oselectivity in good to excellent yields.展开更多
基金The authors would like to thank the National Natural Science Foundation of China(20472083)for financial support.
文摘Two novel monophosphoramidites were synthesized through a five-step transformation from commercially available L-proline. In the Rh-catalyzed asymmetric hydrogenation of α-dehydroamino acid derivatives, ligand （Sc,Rα）-1b showed good enantioselectivity and up to 91% e.e. was obtained.
基金The authors would like to thank the National Natural Science Foundation of China （No. 20472083） for financial support of this work.
文摘Two new C2-symmetrical bidentate phosphoramidite ligands were synthesized and employed in the Rh-catalyzed asymmetric hydrogenation of β-（acylamino）acrylates, up to 89% ee with full conversions was obtained.
基金the support from the National Natural Science Foundation of China(NSFC,Nos.81602954,81573286,81373259 and 81773577).
文摘A new strategy is developed for the synthesis of 1-aminoisoquinoline derivatives.This Rh(III)-catalyzed[4+2]annulation reaction employs benzamidines as efficient directing groups and the vinylene carbonate as an acetylene surrogate.Additionally,the reaction features broad substrate scopes and good yields,only producing carbonate anion as byproduct.
基金the"100 Talent Program of Chinese Academy of Sciences""1000-Youth Talents Plan"+3 种基金ShanghaiYouth Talent,National Science&Technology Major Project"Key New Drug Creation and Manufacturing Program"China(No. 2018ZX09711002–006)Science and Technology Commission of Shanghai Municipality (No. 18431907100)ShanghaiTechnology Innovation Action Plan (No. 18JC1415300)the Research Grants Council of Hong Kong (No. HKUST 16302418) for financial support of this research。
文摘The development of innovative strategies and methods to provide natural product-like macrocycles not accessible by biosynthesis, but endowed with novel bioactivities and simplified structure, is highly desirable. Inspired by the key scaffolds of rapamycin and FR252921, herein, we report a Rh(III)-catalyzed C–H alkylation macrocyclization, which enables access to CF_(3)-substituted macrolides. DFT calculations reveal that the chemoselectivity between C–H alkylation and olefination macrocyclization was highly controllable. Moreover, the unique CF_(3)-substituted macrolides showed potent anti-inflammation activities against TNF-α, IL-6 and CCL2 m RNA expression.
基金Financial support from National Natural Science Foundation of China （Nos. 21162012 and 21362014） and Key Laboratory of Functional Small Organic Mol-ecule, Ministry of Education, Jiangxi Normal University （No. KLFS-KF-201407） is gratefully acknowledged.
文摘A facile and efficient route to 4-aryl-2-[2-（trifluoromethylthio） aryl]quinazoline derivatives through a tandem directed Rh-catalyzed C-H iodination and trifluoromethylthiolation is described. The reaction proceeded under mild reaction conditions, exhibited good functional group tolerance with a broad scope of substrate and excellent regi- oselectivity in good to excellent yields.
