1638677-41-4Relevant academic research and scientific papers
Mild, Aqueous α-Arylation of Ketones: Towards New Diversification Tools for Halogenated Metabolites and Drug Molecules
Marelli, Enrico,Renault, Yohann,Sharma, Sunil V.,Nolan, Steven P.,Goss, Rebecca J. M.
, p. 3832 - 3836 (2017/03/27)
The palladium-catalysed aqueous α-arylation of ketones was developed and tested for a large variety of reaction partners. These mild conditions enabled the coupling of aryl/alkyl-ketones with N-protected halotryptophans, heterocyclic haloarenes, and challenging base-sensitive compounds. The synthetic potential of this new methodology for the diversification of complex bioactive molecules was exemplified by derivatising prochlorperazine. The methodology is mild, aqueous and flexible, representing a means of functionalizing a wide range of halo-aromatics and therefore has the potential to be extended to complex molecule diversification.
LIGAND, NICKEL COMPLEX COMPRISING LIGAND, AND REACTION USING NICKEL COMPLEX
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Paragraph 0282; 0284; 0285, (2016/10/07)
PROBLEM TO BE SOLVED: To provide a method for directly carrying out arylation, especially α-arylation, of a carbonyl compound or a thiocarbonyl compound by using a more inexpensive phenol derivative and a nickel catalyst, and to provide a novel nickel cat
Nickel-catalyzed α-arylation of ketones with phenol derivatives
Takise, Ryosuke,Muto, Kei,Yamaguchi, Junichiro,Itami, Kenichiro
supporting information, p. 6791 - 6794 (2014/07/08)
The nickel-catalyzed α-arylation of ketones with readily available phenol derivatives (esters and carbamates) provides access to useful α-arylketones. For this transformation, 3,4-bis(dicyclohexylphosphino) thiophene (dcypt) was identified as a new, enabling, air-stable ligand for this transformation. The intermediate of an assumed C-O oxidative addition was isolated and characterized by X-ray crystal-structure analysis. The nickel-catalyzed α-arylation of ketones with readily available phenol derivatives (esters and carbamates) provides access to useful α-arylketones. The use of 3,4-bis(dicyclohexylphosphino)thiophene (dcypt) as an air-stable ligand enables this transformation. The intermediate of an assumed C-O oxidative addition was isolated and characterized by X-ray crystal-structure analysis.
