167156-20-9Relevant academic research and scientific papers
Copper-catalyzed formal transfer hydrogenation/deuteration of aryl alkynes
Sloane, Samantha E.,Reyes, Albert,Vang, Zoua Pa,Li, Lingzi,Behlow, Kiera T.,Clark, Joseph R.
supporting information, p. 9139 - 9144 (2020/11/30)
A copper-catalyzed reduction of alkynes to alkanes and deuterated alkanes is described under transfer hydrogenation and transfer deuteration conditions. Commercially available alcohols and silanes are used interchangeably with their deuterated analogues as the hydrogen or deuterium sources. Transfer deuteration of terminal and internal aryl alkynes occurs with high levels of deuterium incorporation. Alkyne-containing complex natural product analogues undergo transfer hydrogenation and transfer deuteration selectively, in high yield. Mechanistic experiments support the reaction occurring through a cis-alkene intermediate and demonstrate the possibility for a regioselective alkyne transfer hydrodeuteration reaction.
Copper-catalyzed and additive free decarboxylative trifluoromethylation of aromatic and heteroaromatic iodides
Johansen, Martin B.,Lindhardt, Anders T.
supporting information, p. 1417 - 1425 (2020/03/03)
A copper-catalyzed decarboxylative trifluoromethylation of (hetero)aromatic iodides has been developed. Importantly, this new copper-catalyzed reaction operates in the absence of any ligands and metal additives. The protocol shows good functional group tolerance and is compatible with heteroaromatic systems. The reaction proved scalable to a 15 mmol scale with increased yield. Finally, late-stage installation of the trifluoromethyl functionality afforded the N-trifluoroacetamide variant of the antidepressant agent, Prozac, demonstrating the applicability of the developed method.
Method for synthesizing benzsulfamide compound from benzene sulfonyl chloride compound and triethylamine without metal catalysis
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Paragraph 0018-0019, (2019/02/04)
The invention relates to a method for synthesizing a benzsulfamide compound from a benzene sulfonyl chloride compound and triethylamine without metal catalysis. The benzsulfamide compound is generatedby adopting the benzene sulfonyl chloride compound and
Rapid and efficient copper-catalyzed finkelstein reaction of (hetero)aromatics under continuous-flow conditions
Chen, Mao,Ichikawa, Saki,Buchwald, Stephen L.
supporting information, p. 263 - 266 (2015/02/05)
A general, rapid, and efficient method for the copper-catalyzed Finkelstein reaction of (hetero)aromatics has been developed using continuous flow to generate a variety of aryl iodides. The described method can tolerate a broad spectrum of functional groups, including N-H and O-H groups. Additionally, in lieu of isolation, the aryl iodide solutions were used in two distinct multistep continuous-flow processes (amidation and Mg-I exchange/nucleophilic addition) to demonstrate the flexibility of this method.
3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: Synthesis and biological evaluation
Lin, Ronghui,Lu, Yanhua,Wetter, Steven K.,Connolly, Peter J.,Turchi, Ignatius J.,Murray, William V.,Emanuel, Stuart L.,Gruninger, Robert H.,Fuentes-Pesquera, Angel R.,Adams, Mary,Pandey, Niranjan,Moreno-Mazza, Sandra,Middleton, Steven A.,Jolliffe, Linda K.
, p. 2221 - 2224 (2007/10/03)
A novel series of 2,6-diamino-3-acylpyridines were designed and synthesized as cyclin-dependent kinase (CDK) inhibitors. The representative compounds 2r and 11 showed potent CDK1 and CDK2 inhibitory activities and inhibited cellular proliferation in HeLa,
