- Selective Late-Stage Hydrodefluorination of Trifluoromethylarenes: A Facile Access to Difluoromethylarenes
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A selective reductive monodefluorination reaction of trifluoromethyl arenes was developed. Mediated by magnesium metal, various difluoromethylated aromatics were accessed at room temperature in the presence of acetic acid. This protocol shows tolerance to a wide range of functional groups and it was applicable in late-stage hydrodefluorination of complex pharmaceutical compounds, affording the corresponding CF2H analogues and their deuterated (CF2D) counterparts.
- Munoz, Socrates B.,Ni, Chuanfa,Zhang, Zhe,Wang, Fang,Shao, Nan,Mathew, Thomas,Olah, George A.,Prakash, G. K. Surya
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p. 2322 - 2326
(2017/05/01)
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- A O-trifluoro methyl process for the preparation of formaldehyde
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The invention discloses a method for preparing o-trifluoromethyl benzaldehyde. The method for preparing the o-trifluoromethyl benzaldehyde, disclosed by the invention, comprises the following steps: in the presence of a catalyst, carrying out hydrolysis reaction on a mixture of o-trifluoromethyl methylbenzene bichloride, o-trifluoromethyl chloro-fluoro-methylbenzene and o-trifluoromethyl methylbenzene difluoride and water at the temperature of 80-150 DEG C to obtain, wherein the mass of the catalyst accounts for 0.01-10% of the mass of the mixture. The method disclosed by the invention is cheap and easily available in raw materials, low in cost, little in wastewater, low in energy consumption and simple in operation and can be suitable for industrial production. The structural formula of the o-trifluoromethyl benzaldehyde is shown in the specification.
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Paragraph 0039; 0040
(2017/02/23)
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- Pd-catalyzed α-arylation of α,α-difluoroketones with aryl bromides and chlorides. A route to difluoromethylarenes
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We report the Pd-catalyzed α-arylation of α,α- difluoroketones with aryl and heteroaryl bromides and chlorides catalyzed by an air- and moisture-stable palladacyclic complex containing P(t-Bu)Cy2 as ligand. The combination of this Pd-catalyzed arylation and base-induced cleavage of the acyl-aryl C-C bond within the α-aryl-α,α- difluoroketone constitutes a one-pot, two-step procedure to synthesize difluoromethylarenes from aryl halides. A broad range of electronically varied aryl and heteroaryl bromides and chlorides underwent these two transformations, providing α-aryl-α,α-difluoroketones, difluoromethylarenes, and difluoromethylheteroarenes in high yields.
- Ge, Shaozhong,Cha?adaj, Wojciech,Hartwig, John F.
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supporting information
p. 4149 - 4152
(2014/04/03)
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- METAL-CATALYZED COUPLING OF ARYL AND VINYL HALIDES WITH ALPHA, ALPHA-DIFLUOROCARBONYL COMPOUNDS
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The coupling of aryl, heteroaryl, and vinyl halides with α,α-difluoroketones or silyl ethers or siylenol ethers of α,α-difluoroketones and α,α-difluoroamides and esters are described. Further derivatization of the coupling products (such as ketone cleavage and Baeyer-Villiger oxidation) is also described.
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Paragraph 0009; 00154-00155
(2014/10/18)
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