- A Unified Catalytic Asymmetric (4+1) and (5+1) Annulation Strategy to Access Chiral Spirooxindole-Fused Oxacycles
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A unified catalytic asymmetric (N+1) (N=4, 5) annulation reaction of oxindoles with bifunctional peroxides has been achieved in the presence of a chiral phase-transfer catalyst (PTC). This general strategy utilizes peroxides as unique bielectrophilic four- or five-atom synthons to participate in the C?C and the subsequent umpolung C?O bond-forming reactions with one-carbon unit nucleophiles, thus providing a distinct method to access the valuable chiral spirooxindole-tetrahydrofurans and -tetrahydropyrans with good yields and high enantioselectivities under mild conditions. DFT calculations were performed to rationalize the origin of high enantioselectivity. The gram-scale syntheses and synthetic utility of the resultant products were also demonstrated.
- Gao, Min,Gong, Xiangnan,Hu, Lin,Luo, Yanshu,Xia, Yuanzhi,Xu, Qianlan,Zhao, Yukun
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supporting information
p. 19813 - 19820
(2021/08/03)
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- Room Temperature Benzofused Lactam Synthesis Enabled by Cobalt(III)-Catalyzed C(sp2)?H Amidation
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Benzofused lactams, especially indolin-2-one and dihydroquinolin-2-one are popular structural motives in durgs and natural products. Herein, we developed a room temperature and robust synthesis of benzofused lactams through cobalt(III)-catalyzed C(sp
- Tian, Xun,Li, Xin,Duan, Shengzu,Du, Ya,Liu, Tongqi,Fang, Yongsheng,Chen, Wen,Zhang, Hongbin,Li, Minyan,Yang, Xiaodong
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p. 1050 - 1058
(2020/12/18)
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- CYCLOHEXYL AMIDE DERIVATIVES AS CRF RECEPTOR ANTAGONISTS
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There are described cydohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists
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Page/Page column 90
(2016/02/02)
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- Non-nucleoside reverse transcriptase inhibitors
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Compounds represented by formula I: wherein R1 is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, and haloalkyl; R2 is H or (C1-4)alkyl; R3 is H or (C1-4)alkyl; R4 is (C1-4)alkyl, (C1-4)alkyl(C3-7)cycloalkyl, or (C3-7)cycloalkyl; and Q is a fused phenyl-5 or 6-membered saturated heterocycle having one to two heteroatoms selected from O and N, said Q being optionally substituted with hydroxy, or (C1-4)alkyl which in turn maybe optionally substituted with pyridinyl-N-oxide or C(O)OR wherein R is H or (C1-4)alkyl; or a salt thereof. The compounds have inhibitory activity against Wild Type, and single and double mutants strains, of HIV.
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- Novel substituted 4-aminomethylpiperidines as potent and selective human β3-agonists. Part 1: Aryloxypropanolaminomethylpiperidines
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The synthesis and SAR of a series of human β3 adrenoreceptor agonists based on a template derived from a common pharmacophore coupled with 4-aminomethylpiperidine is described. Potent and selective agents were identified such as 26 that was in vitro active in CHO cells expressing human β3-AR (EC50=49 nM, IA=1.1), and in vivo active in a transgenic mouse model.
- Steffan, Robert J.,Ashwell, Mark A.,Solvibile, William R.,Matelan, Edward,Largis, Elwood,Han, Stella,Tillet, Jeffery,Mulvey, Ruth
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p. 2957 - 2961
(2007/10/03)
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- A VERSATILE AND EFFICIENT PROCESS TO 3-SUBSTITUTED INDOLES FROM ANILINES
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Borane-mediated reductive elimination of α-thiomethyl-, α-hydroxy-, or α-alkoxy-, α'-substituted oxindoles affords 3-substituted indoles in high yield.Isatins, available via several routes from oxindoles, also afford indoles.
- Wierenga, Wendell,Griffin, John,Warpehoski, Martha A.
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p. 2437 - 2440
(2007/10/02)
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