- Enantioselective Intermolecular C-H Amination Directed by a Chiral Cation
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The enantioselective amination of C(sp3)-H bonds is a powerful synthetic transformation yet highly challenging to achieve in an intermolecular sense. We have developed a family of anionic variants of the best-in-class catalyst for Rh-catalyzed C-H amination, Rh2(esp)2, with which we have associated chiral cations derived from quaternized cinchona alkaloids. These ion-paired catalysts enable high levels of enantioselectivity to be achieved in the benzylic C-H amination of substrates bearing pendant hydroxyl groups. Additionally, the quinoline of the chiral cation appears to engage in axial ligation to the rhodium complex, providing improved yields of product versus Rh2(esp)2 and highlighting the dual role that the cation is playing. These results underline the potential of using chiral cations to control enantioselectivity in challenging transition-metal-catalyzed transformations.
- Fanourakis, Alexander,Paterson, Kieran J.,Phipps, Robert J.,Williams, Benjamin D.
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supporting information
p. 10070 - 10076
(2021/07/21)
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- 3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 00484
(2017/10/06)
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- Amine compound and a manufacturing method thereof, and use thereof
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PROBLEM TO BE SOLVED: To provide a material for an organic EL developing a higher efficiency than conventional materials, and a material very useful particularly in an organic EL device using a phosphorescent material. SOLUTION: The material is an a
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Paragraph 0075; 0076
(2020/07/01)
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- TETRAHYDROISOQUINOLINE COMPOUND
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The present invention relates a specific tetrahydroisoquinoline compound which is useful as a chemokine receptor type 3 (CCR3) antagonist, and a pharmaceutical composition comprising the same as an active ingredient. The tetrahydroisoquinoline compound of the present invention is useful for the treatment or prevention of a disease in which CCR3 participates.
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Page/Page column 61-62
(2010/01/29)
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- THIAZOLOPYRIMIDINONE DERIVATIVES AS PI3 KINASE INHIBITORS
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This invention relates to the use of thiazolopyrimidinone derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3' OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ
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Page/Page column 42-43
(2010/12/18)
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- Rational modification of a candidate cancer drug for use against chagas disease
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Chagas disease is one of the major neglected diseases of the world. Existing drug therapies are limited, ineffective, and highly toxic. We describe a novel strategy of drug discovery of adapting an existing clinical compound with excellent pharmaceutical properties to target a pathogenic organism. The protein farnesyltransferase (PFT) inhibitor tipifarnib, now in phase III anticancer clinical trials, was previously found to kill Trypanosoma cruzi by blocking sterol 14a-demethylase (14DM). We rationally developed tipifarnib analogues that display reduced affinity for human PFT to reduce toxicity while increasing affinity for parasite 14DM. The lead compound has picomolar activity against cultured T. cruzi and is efficacious in a mouse model of acute Chagas disease.
- Kraus, James M.,Verlinde, Christophe L. M. J.,Karimi, Mandana,Lepesheva, Galina I.,Gelb, Michael H.,Buckner, Frederick S.
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scheme or table
p. 1639 - 1647
(2010/01/07)
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- ARYL FLUOROETHYL UREAS ACTING AS ALPHA 2 ADRENERGIC AGENTS
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The invention provides well-defined aryl fluoroethyl ureas that are useful as selective alpha2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of alpha2 adrenergic receptors.
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- INHIBITORS OF MONOAMINE UPTAKE
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N,N-disubstituted 4-amino-piperidines of the general Formula (I) are inhibitors of the uptake of serotonin and/or norepinephrine and/or dopamine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.
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- Syntheses and Reactions of the First Dithiametacyclophanes, Metacyclophanes, and Metacyclophanedienes
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Two new cyclophane series, the dithiametacyclophanes 5 and the metacyclophanedienes 6, are synthesized and their chemistry is described.On the basis of this chemistry, such cyclophanes appear not to adopt the syn or anti conformations fo
- Mitchell, Reginald H.,Lai, Yee-Hing
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p. 2534 - 2540
(2007/10/02)
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