1246025-07-9

Upstream product

• 1514-82-5 2-bromo-3,3,3-trifluoropropene 
• 104-87-0 4-methyl-benzaldehyde 
• 122-00-9 para-methylacetophenone 

Downstream Products

• 1246025-12-6 (R)-4,4,4-trifluoro-3-(1H-indol-3-yl)-1-p-tolylbutan-1-one 
• 331943-04-5 4-[3-(4-methylphenyl)-5-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide 

Relevant academic research and scientific papers

Rh-Catalyzed C-H alkylation enabling modular synthesis of CF3-substituted benzannulated macrocyclic inhibitors of B cell responses

Inspired by aspirin and chalcone, herein, we describe a modular biomimetic strategy to achieve a new class of CF3-bearing benzannulated macrolactams. The key to the success of macrolactams was the utilization of a highly chemoselective Rh(iii)-catalyzed native carboxylic acid-directed C-H alkylation. Moreover, the unique CF3-containing benzannulated macrocycles showed decent immunosuppressive effects on B cellsin vitro, including proliferation, activation, and antibody production upon specific stimulation implicating TLR and BCR signaling.

Oxidation of 4-Aryl-1,1,1-trifluorobut-2-en-2-yl Trifluoro?-methanesulfonates by 4-Picoline-N-Oxide: A Novel Approach to β-Trifluoromethyl-α,β-enones

An efficient approach to β-trifluoromethyl-α,β-enones via oxidation of 4-aryl-1,1,1-trifluorobut-2-en-2-yl trifluoromethanesulfonates is described. The reaction proceeds smoothly under mild and metal?-free conditions and tolerates a wide range of functional groups. Various β-trifluoromethyl-α,β-enones were obtained in moderate to good yields.

Preparation method of (E)-1-aryl-4, 4, 4-trifluorobutyl-2-ene-1-one compound

The invention discloses a preparation method of an (E)-1-aryl-4, 4, 4-trifluorobutyl-2-ene-1-one compound, and belongs to the field of compound preparation. The (E)-1-aryl-4, 4, 4-trifluorobutyl-2-ene-1-one compound is prepared by taking a compound shown

Lewis Acid-Catalyzed Rearrangement of Fluoroalkylated Propargylic Alcohols: An Alternative Approach to β-Fluoroalkyl-α,β-enones

A practical Lewis acid-catalyzed Meyer-Schuster rearrangement of fluoroalkylated propargylic alcohols, leading to a series of β-fluoroalkyl-α,β-enones, is developed. The methodology reported herein features moderate to high yields and high stereoselectivi

Rh(III)-Catalyzed [3 + 2] Annulation via C-H Activation: Direct Access to Trifluoromethyl-Substituted Indenamines and Aminoindanes

The rhodium(III)-catalyzed direct C-H addition and annulation of benzimidates and aldimines with β-(trifluoromethyl)-α,β-unsaturated ketones is described. This protocol provides the facile and efficient formation of various trifluoromethyl-containing inde

Chiral Hydroxytetraphenylene-Catalyzed Asymmetric Conjugate Addition of Boronic Acids to Enones

(S)-2,15-Br2-DHTP-catalyzed asymmetric conjugate addition of boronic acids to β-trifluoromethyl α,β-unsaturated ketones and enones was studied. The reaction afforded the corresponding Michael addition products in moderate to high yields with excellent enantioselectivities (up to 99:1 er). This catalytic system features mild reaction conditions, high efficiency, and tolerance to heteroarylboronic acids.

Rhodium(III)-catalyzed sp2 C-H bond addition to CF3-substituted unsaturated ketones

Rhodium(iii)-catalyzed conjugate addition of aromatic and olefinic C-H bonds to CF3-substituted unsaturated ketones was efficiently achieved. Both arene and olefin substrates bearing a chelate assisted-directing group were coupled with a variet

Isothiourea-mediated one-pot synthesis of functionalized pyridines

Acids to bases: The synthesis of 2,4,6-trisubstituted pyridines from (phenylthio)acetic acid and a range of α,β-unsaturated ketimines is reported. This process proceeds by intermolecular Michael addition/ lactamization, thiophenol elimination, and N- to O

Synthesis of functionalized indoles with a trifluoromethyl-substituted stereogenic tertiary carbon atom through an enantioselective Friedel-Crafts alkylation with β-trifluoromethyl-α,β-enones

Chiral complexes of BINOL-based ligands with zirconium tert-butoxide catalyze the Friedel-Crafts alkylation reaction of indoles with β-trifluoromethyl-α,β-unsaturated ketones to give functionalized indoles with an asymmetric tertiary carbon center attached to a trifluoromethyl group. The reaction can be applied to a large number of substituted α-trifluoromethyl enones and substituted indoles. The expected products were obtained with good yields and ees of up to 99%.