350490-15-2Relevant academic research and scientific papers
Selective Construction of C?C and C=C Bonds by Manganese Catalyzed Coupling of Alcohols with Phosphorus Ylides
Liu, Xin,Werner, Thomas
supporting information, p. 1096 - 1104 (2020/12/31)
Herein, we report the manganese catalyzed coupling of alcohols with phosphorus ylides. The selectivity in the coupling of primary alcohols with phosphorus ylides to form carbon-carbon single (C?C) and carbon-carbon double (C=C) bonds can be controlled by the ligands. In the conversion of more challenging secondary alcohols with phosphorus ylides the selectivity towards the formation of C?C vs. C=C bonds can be controlled by the reaction conditions, namely the amount of base. The scope and limitations of the coupling reactions were thoroughly evaluated by the conversion of 21 alcohols and 15 ylides. Notably, compared to existing methods, which are based on precious metal complexes as catalysts, the present catalytic system is based on earth abundant manganese catalysts. The reaction can also be performed in a sequential one-pot reaction generating the phosphorus ylide in situ followed manganese catalyzed C?C and C=C bond formation. Mechanistic studies suggest that the C?C bond was generated via a borrowing hydrogen pathway and the C=C bond formation followed an acceptorless dehydrogenative coupling pathway. (Figure presented.).
AMIDE COMPOUND HAVING BET PROTEOLYSIS-INDUCING ACTION AND MEDICINAL APPLICATION THEREOF
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Paragraph 0540-0542, (2020/01/31)
The present invention aims to provide a compound that: has an excellent cytotoxic action on cancer cells, excellent induction of BET protein degradation in cancer cells, and an excellent binding-inhibiting action on BET protein and acetylated histone; and is effective as an anti-cancer agent, a BET protein degradation-inducing agent, or a BET protein inhibiting agent. A compound indicated in general formula (I) or a pharmacologically acceptable salt thereof. {In the formula, each symbol is as outlined in the Description.}
Propionic Acid Derivatives and Methods of Use Thereof
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Paragraph 1834; 1835, (2018/11/21)
Provided herein are compounds and pharmaceutical compositions of formula I where R1, R2, R3, R4, R5 and R6 are as described herein. Also provided pharmaceutically acceptable salts or stereoisomers of these compounds. In addition methods are provided for inhibiting the binding of an integrin to treat various pathophysiological conditions.
PROCESS FOR THE PREPARATION OF (E)-3-(4-((E)-2-(2-CHLORO-4-FLUOROPHENYL)-1-(1H-INDAZOL-5-YL)BUT-1-EN-1-YL)PHENYL)ACRYLIC ACID
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Page/Page column 30; 31, (2017/05/07)
Processes are described for the preparation of estrogen receptor modulating compound, (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid (I): and salts thereof, and intermediates useful for the preparation of (I).
Improving reactivity and selectivity of aqueous-based Heck reactions by the local hydrophobicity of phosphine ligands
Roberts, Gina M.,Zhang, Shiyong,Zhao, Yan,Woo, L. Keith
, p. 8263 - 8270 (2015/10/05)
Modification of a triarylphosphine with a cholate moiety affords a new ligand, 1, which is effective in palladium-catalyzed Heck cross-couplings between acrylates and aryl iodides under mild, aqueous reaction conditions. High yields, up to 99%, were achieved in water at 40 °C. In competition studies, a more hydrophobic substrate (n-Bu acrylate) was preferred over the least hydrophobic substrate (methyl acrylate), supportive of a localized hydrophobic microenvironment near the catalytic center. The enhanced reactivity and selectivity for hydrophobic substrates disappeared when the local hydrophobicity was eliminated using a standard water-soluble phosphine or in organic solvents.
A chiral ligand mediated aza-conjugate addition strategy for the enantioselective synthesis of β-amino esters that contain hydrogenolytically sensitive functionality
Archer, Robert M.,Hutchby, Marc,Winn, Caroline L.,Fossey, John S.,Bull, Steven D.
, p. 8838 - 8847 (2015/10/20)
Aza-conjugate addition of the lithium anion of N-trimethylsilyl-p-methoxybenzylamine to tert-butyl enoate acceptors, in the presence of a stoichiometric amount of enantiopure 1,2-dimethoxy-1,2-diphenylethane and excess trimethylsilyl chloride, affords ter
Organocatalytic deprotonative functionalization of C(sp2)-H and C(sp3)-H bonds using in situ generated onium amide bases
Inamoto, Kiyofumi,Okawa, Hitomi,Taneda, Hiroshi,Sato, Maomi,Hirono, Yutaro,Yonemoto, Misato,Kikkawa, Shoko,Kondo, Yoshinori
supporting information, p. 9771 - 9773,3 (2020/08/31)
Onium amides, generated in situ from the combination of aminosilanes and onium fluorides (R4PF, R4NF), are employed for the first time as bases for catalytic deprotonative functionalization of C(sp 2)-H and activated C(sp
Processes for Preparing 1,2-Substituted Cyclopropyl Derivatives
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Page/Page column 9, (2012/04/04)
The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceut
Palladium-catalyzed C-C bond formation of arylhydrazines with olefins via carbon-nitrogen bond cleavage
Zhu, Ming-Kui,Zhao, Jun-Feng,Loh, Teck-Peng
supporting information; experimental part, p. 6308 - 6311 (2012/01/06)
The unactivated carbon-nitrogen bond of various aryl hydrazines was cleaved under very mild conditions by Pd(0) with the assistance of Pd(II). The in situ generated aryl palladium complex readily takes part in the C-C bond formation with olefins. This study offered a new mode of C-Pd bond formation, which will spur the development of palladium-catalyzed cross-coupling in the future.
Cyclopropyl Amide Derivatives 978
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Page/Page column 35, (2009/04/24)
Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclo
