- Expanding the Boundaries of Water-Tolerant Frustrated Lewis Pair Hydrogenation: Enhanced Back Strain in the Lewis Acid Enables the Reductive Amination of Carbonyls
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The development of a boron/nitrogen-centered frustrated Lewis pair (FLP) with remarkably high water tolerance is presented. As systematic steric tuning of the boron-based Lewis acid (LA) component revealed, the enhanced back-strain makes water binding increasingly reversible in the presence of relatively strong base. This advance allows the limits of FLP's hydrogenation to be expanded, as demonstrated by the FLP reductive amination of carbonyls. This metal-free catalytic variant displays a notably broad chemoselectivity and generality.
- Dorkó, éva,Szabó, Márk,Kótai, Bianka,Pápai, Imre,Domján, Attila,Soós, Tibor
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supporting information
p. 9512 - 9516
(2017/08/01)
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- HAT INHIBITORS AND METHODS FOR THEIR USE
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Compounds having a structure of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b, R3a, R3b, R3c, R4a, R4b, R5, R6, Z and X are as defined herein are provided. Pharmaceutical compositions comprising such compounds and methods for treating various HAT-related conditions or diseases, including cancer, by administration of such compounds are also provided.
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Page/Page column 49
(2016/04/10)
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- SPIROCYCLIC HAT INHIBITORS AND METHODS FOR THEIR USE
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Compounds having a structure of Formula (IX) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, Q1----Q2, R6, R7, A, B, W, x, and y are as defined herein and are provided. Pharmaceutical compositions comprising such compounds and methods for treating various HAT-related conditions or diseases, including cancer, by administration of such compounds are also provided.
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Page/Page column 538
(2016/04/10)
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- A simple and efficient preparation of 3,4-dialkylsubstituted tetrahydroisoquinoline using cyclopropylethyliden benzylamine
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Intramolecular Friedel-Crafts alkylation of N-benzyl-N-(1-cyclopropylethyl)acetamide to 3,4-dialkyl substituted tetrahydroisoquinoline by reaction of the acetamide with an excess of PPA is described. The conformational study of intermediates by high resol
- Kouznetsov, Vladimir,Palma, Alirio,Rozo, Wilson,Stashenko, Elena,Bahsas, Ali,Amaro-Luis, Juan
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p. 2965 - 2971
(2007/10/03)
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- Hydrozirconation of alkenyloxirane derivatives: Preparation of cycloalkylmethanols
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Cyclopentyl and cyclopropylmethanol derivatives were efficiently prepared through a chemoselective hydrozirconation reaction of (1- butenyl)oxirane and vinyloxirane with Cp2ZrHCl. However, the attemped reaction of (1-pentenyl)oxirane or (1-propenyl)oxirane failed to yield cyclohexyl or cyclobutylmethanols. The ring formation was stereospecific and proceeded with the inversion of the configuration at the reacting oxirane carbon. The origin of stereospecificity and the stereoselectivity in the formation of cyclopropylmethanols was presumed by the approach of the Schwartz reagent from the less hindered site of the stable gauche-conformer of the vinyloxirane compound in the transition state. (Cyclopropylmethyl)amine derivatives were also prepared by the treatment of vinylaziridine derivatives with Cp2ZrHCl.
- Harada, Susumu,Kowase, Noboru,Tabuchi, Nobuhito,Taguchi, Takeo,Dobashi, Yasuo,Dobashi, Akira,Hanzawa, Yuji
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p. 753 - 766
(2007/10/03)
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