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Upstream product

• 75-88-7 1,1,1-trifluoro-2-chloroethane 
• 99-02-5 3'-Chloroacetophenone 
• 2142-63-4 1-(3-Bromophenyl)ethanone 
• 353-83-3 1,1,1-trifluoro-2-iodoethane 
• 14452-30-3 3'-iodoacetophenone 
• 373-88-6 2,2,2-trifluroethylamine hydrochloride 
• 214360-49-3 1-[3-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl]-ethanone 

Relevant academic research and scientific papers

Using Chlorotrifluoroethane for Trifluoroethylation of (Hetero)aryl Bromides and Chlorides via Nickel Catalysis

A nickel-catalyzed reductive cross-coupling between industrial chemical CF3CH2Cl and (hetero)aryl bromides and chlorides has been reported. The reaction is synthetically simple without the preparation of arylmetals and exhibits high functional group tolerance. The utility of this protocol has been demonstrated by the late-stage modification of pharmaceuticals, providing a facile route for medicinal chemistry.

Nickel-Catalyzed Direct Trifluoroethylation of Aryl Iodides with 1,1,1-Trifluoro-2-Iodoethane via Reductive Coupling

A nickel-catalyzed direct trifluoroethylation of aryl iodides with an industrial raw material CF3CH2I has been developed, demonstrating high efficiency, excellent functional-group compatibility, especially with large sterically hindered groups. The key to success is the combination of nickel with readily available nitrogen and phosphine ligands. The powerful potential of this strategy is further demonstrated by the late-stage modification of several derived bioactive molecules. (Figure presented.).

Preparation method of trifluoroethyl compounds

The invention discloses a preparation method of trifluoroethyl compounds. The trifluoroethyl compounds are synthesized by directly using cheap and abundant industrial raw materials 2-chloro-1,1,1-trifluoroethane and halogenated substances as raw materials by stirring in a polar solvent under the action of a catalytic system using cheap and an easily available alkali metal nickel salt catalyst anda pyridine ligand for reacting under mild reaction conditions of 50-90 DEG C for 12-24 hours, and the efficient introduction of the trifluoroethyl groups to aromatic ring groups or heterocyclic aryl groups can be realized to prepare the trifluoroethyl compounds. The method has the advantages of mild reaction conditions, simple operation, low cost of raw materials and catalysts, good compatibilityof substrate functional groups, easy expansion of reaction scale, simple separation of products and suitability for industrial production.

ANTICANCER COMBINATION THERAPY

The invention describes anti-cancer therapies comprising using a SOS1 inhibitor in combination with a MEK inhibitor, each as described herein.

Exploiting the trifluoroethyl group as a precatalyst ligand in nickel-catalyzed Suzuki-type alkylations

We report herein the exploitment of the partially fluorinated trifluoroethyl as precatalyst ligands in nickel-catalyzed Suzuki-type alkylation and fluoroalkylation coupling reactions. Compared with the [LnNiII(aryl)(X)] precatalysts, the unique characters of bis-trifluoroethyl ligands imparted precatalyst [(bipy)Ni(CH2CF3)2] with bench-top stability, good solubilities in organic media and interesting catalytic activities. Preliminary mechanistic studies reveal that an eliminative extrusion of a vinylidene difluoride (VDF, CH2CF2) mask from [(bipy)Ni(CH2CF3)2] is a critical step for the initiation of a catalytic reaction.

NOVEL BENZYLAMINO SUBSTITUTED PYRIDOPYRIMIDINONES AND DERIVATIVES AS SOS1 INHIBITORS

The present invention encompasses compounds of formula (I) wherein the groups R1 to R4, A and p have the meanings given in the claims and specification, their use as inhibitors of SOS1, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

Switchable 2,2,2-trifluoroethylation and gem-difluorovinylation of organoboronic acids with 2,2,2-trifluorodiazoethane

The transition-metal-free 2,2,2-trifluoroethylation and gem-difluorovinylation of arylboronic acids were developed. By employing different reaction conditions, these transformations provide both (2,2,2-trifluoroethyl)arenes and gem-difluorovinylarenes fro

The palladium-catalyzed cross-coupling reactions of trifluoroethyl iodide with aryl and heteroaryl boronic acid esters

The cross-coupling reactions of 1,1,1-trifluoro-2-iodoethane with aryl and heteroaryl boronic acid esters have been successfully achieved. The new protocol allows for a convenient introduction of trifluoroethyl groups into a variety of aryl and heteroaryl moieties under mild conditions.

Palladium-catalyzed 2,2,2-trifluoroethylation of organoboronic acids and esters

Trifluoroethylation: Aryl boronic acids can be catalytically trifluoroethylated with the readily available reagent CF3CH 2I (see scheme, dba=dibenzylideneacetone). The reaction tolerates a variety of functional groups and can be extended to the trifluoroethylation of aryl or alkenyl boronic esters. The method is also suitable for the late-stage installation of the CF3CH2 group into target molecules. Copyright