50562-05-5

Upstream product

• 17933-03-8 m-tolylboronic acid 
• 1711-06-4 3-Methylbenzoyl chloride 
• 135754-82-4 3-methyl-N-methoxy-N-methylbenzamide 
• 454-31-9 ethyl difluoroacetate 
• 591-17-3 meta-bromotoluene 
• 585-74-0 3-Methylacetophenone 
• 53764-99-1 4,4,4-trifluoro-1-(3-methylbenzene)butane-1,3-dione 

Downstream Products

• 50562-12-4 1-(m-Tolyl)-2,2-difluorethanol 

Relevant academic research and scientific papers

Biocatalytic Strategy for the Highly Stereoselective Synthesis of CHF2-Containing Trisubstituted Cyclopropanes

The difluoromethyl (CHF2) group has attracted significant attention in drug discovery and development efforts, owing to its ability to serve as fluorinated bioisostere of methyl, hydroxyl, and thiol groups. Herein, we report an efficient biocat

N-phenyl-N-p-toluenesulfonyl difluoroacetamide and application thereof

The invention belongs to the field of pharmaceutical and chemical intermediates and relative chemical technologies. N-phenyl-N-p-toluenesulfonyl difluoroacetamide and application thereof are disclosed. Under the action of a metal catalyst, a ligand and alkali, N-phenyl-N-p-toluenesulfonyl difluoroacetamide, which is used as a difluoroacetylation reagent, reacts with an arylboronic acid compound inan organic solvent to be efficiently and highly selectively converted into a difluoroacetophenone compound. The synthetic method of the difluoroacetophenone compound has few reaction steps, is environmentally-friendly by using stable, easily-stored and cheap and easily-available NDFTS as the difluoroacetyl source, has mild reaction condition, and is convenient to operate; and since the target product is obtained with high yield and high selectivity, the synthetic method has good industrial production value and practical application value. The difluoroacetophenone compound synthesized by the method can be further subjected to a functionalization reaction and is widely applied in the fields of medicine, pesticide, bioactive molecule and functional material molecule synthesis.

Synthesis of Difluoromethyl Ketones from Weinreb Amides, and Tandem Addition/Cyclization of o-Alkynylaryl Weinreb Amides

[Difluoro(phenylsulfanyl)methyl]trimethylsilane (PhSCF2SiMe3) underwent a fluoride-induced nucleophilic addition to the carbonyl group of Weinreb amides to provide the corresponding difluoro(phenylsulfanyl)methyl ketones. These were

Catalytic Enantioselective Synthesis of Highly Functionalized Difluoromethylated Cyclopropanes

The first catalytic asymmetric synthesis of highly functionalized difluoromethylated cyclopropanes is described. The method, based on a rhodium-catalyzed cyclopropanation of difluoromethylated olefins, gives access to a broad range of cyclopropanes bearing ester, ketone, or nitro functional groups. By using Rh2((S)-BTPCP)4 as a catalyst, the corresponding products were obtained in high yields and high diastereo- and enantioselectivities (up 20:1 d.r. and 99 % ee). This methodology allowed preparation of enantioenriched difluoromethylcyclopropanes for the first time.

One-pot synthesis of difluoromethyl ketones by a difluorination/fragmentation process

Difluoromethyl ketones are an under-studied class of ketones which have great potential as useful building blocks for materials and drug design. Here we report a simple and convenient synthesis of this class of compounds via a one-pot difluorination/fragm