51638-15-4

Upstream product

• 2967-66-0 methyl 4-(trifluoromethyl)benzoate 
• 756-79-6 dimethyl methane phosphonate 

Downstream Products

• 951231-33-7 (E)-3-cyclopropyl-1-(4-trifluoromethyl-phenyl)-propenone 
• 1399822-32-2 dimethyl [2-hydroxy-2-(4-trifluoromethylphenyl)ethyl]phosphonate 
• 1415922-84-7 dimethyl (1-acetamido-2-oxo-2-(4-(trifluoromethyl)phenyl)ethyl)phosphonate 
• 1415922-52-9 dimethyl (1-acetamido-2-hydroxy-2-(4-(trifluoromethyl)phenyl)ethyl)phosphonate 
• 75380-98-2 C₁₂H₁₁F₃O₃ 

Relevant academic research and scientific papers

Highly Chemo- And Enantioselective Hydrogenation of 2-Substituted-4-oxo-2-alkenoic Acids

The highly chemo- and enantioselective hydrogenation of (E)-2-substituted-4-oxo-2-alkenoic acids was established for the first time using the Rh/JosiPhos complex, affording a series of chiral α-substituted-γ-keto acids with excellent results (up to 99% yield and >99% ee) and high efficiency (up to 3000 TON). In addition, the importance of this methodology was further demonstrated by a concise and gram-scale synthesis of the anti-inflammatory drug (R)-flobufen.

Access to chiral α-substituted-β-hydroxy arylphosphonates enabled by biocatalytic dynamic reductive kinetic resolution

Ketoreductase (KRED)-catalyzed dynamic reductive kinetic resolution (DYRKR) of α-substituted-β-keto arylphosphonates was developed as a generic and stereoselective approach to synthesize chiral α-substituted-β-hydroxy arylphosphonates, with moderate-to-excellent isolated yield (up to 96%), good-to-excellent diastereoselectivity (up to >99 : 99% ee) being achieved.

Diastereo- and enantioselective asymmetric hydrogenation of α-amido-β-keto phosphonates via dynamic kinetic resolution

Dynamic kinetic resolution of various α-amido-β-keto phosphonates via asymmetric hydrogenation proceeded efficiently to give the corresponding β-hydroxy-α-amido phosphonates in high diastereo- and enantioselectivities (up to 99:1 syn/anti, 99.8% ee). The addition of catalytic amounts of CeCl3 3 7H2O is necessary to achieve both good selectivity and catalytic efficiency under mild reaction conditions.

A practical preparation of aryl β-ketophosphonates

The condensation of alkyl phosphonates with aryl esters to give β-ketophosphonates may be carried out at elevated temperatures mediated by LiHMDS under Barbier type conditions. The reaction is scalable, does not require specialized cryogenic equipment, and is general for all aryl and heteroaryl esters examined.

PYRIDINE AND PYRIMIDINE DERIVATIVES AS MGIUR2 ANTAGONISTS

The present invention relates to compounds of formula (I), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders:wherein A, B, X, Y, R1, R2, R3 and R4 are as defined in the description and claims.