90369-76-9Relevant academic research and scientific papers
Enantioselective Intermolecular C-H Amination Directed by a Chiral Cation
Fanourakis, Alexander,Paterson, Kieran J.,Phipps, Robert J.,Williams, Benjamin D.
supporting information, p. 10070 - 10076 (2021/07/21)
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.
Amine compound and a manufacturing method thereof, and use thereof
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Paragraph 0075;0077, (2020/07/01)
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
THIAZOLOPYRIMIDINONE DERIVATIVES AS PI3 KINASE INHIBITORS
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Page/Page column 43, (2010/12/18)
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
Rational modification of a candidate cancer drug for use against chagas disease
Kraus, James M.,Verlinde, Christophe L. M. J.,Karimi, Mandana,Lepesheva, Galina I.,Gelb, Michael H.,Buckner, Frederick S.
scheme or table, p. 1639 - 1647 (2010/01/07)
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.
Synthesis, reactions, and structural and NMR features of [2.2]metacyclophane monoenes and their tricarbonylchromium and cyclopentadienyliron(+) complexes
Mitchell, Reginald H.,Zhang, Limin
, p. 7140 - 7152 (2007/10/03)
8,16-Dimethyl-, 5,8,13,16-tetramethyl-, and 4,6,8,12,14,16- hexamethyl[2.2]metacyclophanene have been synthesized from the corresponding methyl-substituted 3-thia[3.2]metacyclophane precursors via a Wittig rearrangement-Hofmann elimination procedure. Simp
Syntheses and Reactions of the First Dithiametacyclophanes, Metacyclophanes, and Metacyclophanedienes
Mitchell, Reginald H.,Lai, Yee-Hing
, p. 2534 - 2540 (2007/10/02)
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
