1601477-00-2

Upstream product

• 421-50-1 1,1,1-trifluoro-2-propanone 
• 1576-35-8 toluene-4-sulfonic acid hydrazide 

Downstream Products

• 864737-08-6 1-(benzyloxy)-3-(3,3,3-trifluoroprop-1-en-2-yl)benzene 
• 1601477-36-4 N-(4-(3,3,3-trifluoroprop-1-en-2-yl)phenyl)acetamide 
• 1601477-37-5 phenyl(2-(3,3,3-trifluoroprop-1-en-2-yl)phenyl)methanone 
• 1601477-38-6 2-(3-(3,3,3-trifluoroprop-1-en-2-yl)phenyl)-1,3-dioxolane 
• 91-20-3 naphthalene 
• 136476-29-4 2-(α-(trifluoromethyl)ethenyl)naphthalene 
• 1256366-80-9 1-phenoxy-4-(3,3,3-trifluoroprop-1-en-2-yl)benzene 
• 136476-23-8 1-(4-(3,3,3-trifluoroprop-1-en-2-yl)phenyl)ethan-1-one 
• 471856-97-0 4-(1,1,1-trifluoroprop-2-en-2-yl)benzonitrile 
• 893738-51-7 3-(3,3,3-trifluoroprop-1-en-2-yl)benzaldehyde 
• 1261137-92-1 1,2-dichloro-4-(3,3,3-trifluoroprop-1-en-2-yl)benzene 
• 136476-26-1 2-(3,3,3-trifluoroprop-1-en-2-yl)benzaldehyde 

Relevant academic research and scientific papers

A general synthesis of α-trifluoromethylstyrenes through palladium-catalyzed cross-couplings with 1,1,1-trifluoroacetone tosylhydrazone

1,1,1-Trifluoroacetone tosylhydrazone is presented as a very convenient substrate for the palladium-catalyzed cross-coupling with aryl halides. Under the proper reaction conditions, 3,3,3-trifluoromethylstyrenes - very valuable trifluoromethylated synthetic intermediates - are obtained with high yields. The reaction features a very wide scope, as the presence of most functional groups is tolerated. Moreover, the reaction has been extended to substituted trifluoromethylstyrenes by employing substituted tosylhydrazones derived from other trifluoromethyl ketones.

Organocatalytic Enantioselective Synthesis of Trifluoromethyl-Containing Tetralin Derivatives by Sequential (Hetero)Michael Reaction–Intramolecular Nitrone Cycloaddition

The enantioselective synthesis of tetralin derivatives bearing a trifluoromethylated all-carbon quaternary stereocenter has been accomplished through a synthetic sequence comprising an organocatalytic β-functionalization of ortho-1-trifluoromethylvinyl-(hetero)aromatic conjugated aldehydes followed by the intramolecular nitrone 1,3-cycloaddition reaction (INCR). Both nitromethane and N-Cbz-hydroxylamine were employed as nucleophiles in the initial organocatalytic conjugate addition step, which provided the chiral information required for the subsequent diastereoselective INCR. Although diastereoselectivity was moderate, good yields and enantioselectivities were, in general, obtained. Interestingly, an inversion of the selectivity in the intramolecular cycloaddition step was observed when either nitromethane or N-Cbz-hydroxylamine was employed. This outcome was studied by means of theoretical calculations, which were in agreement with the experimental results. In addition, the ring opening of the isoxazolidine moiety furnished the corresponding fluorinated diamino alcohols in a very efficient manner. (Figure presented.).

N-(PYRIDIN-2-YLSULFONYL)CYCLOPROPANECARBOXAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF A CFTR MEDIATED DISEASE

The invention relates to heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.

Asymmetric Allylation/RCM-Mediated Synthesis of Fluorinated Benzo-Fused Bicyclic Homoallylic Amines As Dihydronaphthalene Derivatives

Enantiomerically enriched fluorinated benzo-fused bicyclic homoallylic amines have been synthesized through an asymmetric allylation/ring closing metathesis (RCM) sequence. This sequence has been carried out using α-trifluoromethylstyrene derivatives as key intermediates, synthesized by microwave radiation. The great deactivating effect exerted by such substituents has been brought to light by a comparative study.

Pd-carbene migratory insertion: Application to the synthesis of trifluoromethylated alkenes and dienes

Pd-catalyzed cross-coupling of halides with CF3-substituted diazo compounds or N-tosylhydrazones has been explored for the synthesis of CF3-substituted alkenes and 1,3-butadienes. Pd-carbene migratory insertion plays the key role in these transformations. Copyright