669074-41-3

Upstream product

• 90719-32-7 (S)-4-Benzyl-2-oxazolidinone 
• 406-93-9 4,4,4-trifluorobutyric acid 
• 2314-97-8 iodotrifluoromethane 
• 90719-27-0 (S)-3-acryloyl-4-benzyloxazolidin-2-one 

Downstream Products

• 1532540-54-7 (4S)-4-benzyl-3-[(2S,3R,E)-3-hydroxy-5-phenyl-2-(2,2,2-trifluoroethyl)pent-4-enoyl]oxazolidin-2-one 
• 1532540-55-8 (4S)-4-benzyl-3-[(2R,3S,E)-3-hydroxy-5-phenyl-2-(2,2,2-trifluoroethyl)pent-4-enoyl]oxazolidin-2-one 
• 1532540-52-5 (4S)-4-benzyl-3-[(2S,3R,E)-3-hydroxy-2-(2,2,2-trifluoroethyl)hex-4-enoyl]oxazolidin-2-one 
• 1532540-50-3 (4S)-4-benzyl-3-[(2S,3R)-3-hydroxy-2-(3,3,3-trifluoropropyl)pent-4-enoyl]oxazolidin-2-one 

Relevant academic research and scientific papers

Synthesis of enantiomerically pure (2S,3S)-5,5,5-trifluoroisoleucine and (2R,3S)-5,5,5-trifluoro-allo-isoleucine

A practical route for the stereoselective synthesis of (2S,3S)-5,5,5- trifluoroisoleucine (L-5-F3Ile) and (2R,3S)-5,5,5-trifluoro-alloisoleucine (D-5-F3-allo-Ile) was developed. The hydrophobicity of L-5-F3Ile was examined and it was incorporated into a m

CYCLIC TETRAMER COMPOUNDS AS PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDERS

The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R1, R1, R1, R1, R1, R1, R1, R1, R1, X1, X2, and X3 are described herein.

Conjugate hydrotrifluoromethylation of α,β-unsaturated acyl-oxazolidinones: Synthesis of chiral fluorinated amino acids

A novel conjugate hydrofluoroalkylation of α,β-unsaturated acyl-oxazolidinones is described. Using this method, enantiomerically pure β-trifluoromethylated amino acids were prepared. Trifluorovaline and trifluoroisoleucine were incorporated into peptides and found to show extremely low α-helix propensities.

P3 cap modified Phe*-Ala series BACE inhibitors

With the aim of reducing molecular weight and adjusting log D value of BACE inhibitors to more favorable range for BBB penetration and better bioavailability, we synthesized and evaluated several series of P3 cap modified BACE inhibitors obtained via replacement of the P3 NHBoc moiety as seen in 3 with other polar functional groups such as amino, hydroxyl and fluorine. Several promising inhibitors emerging from this P3 cap SAR study (e.g., 15 and 19) demonstrated good enzyme inhibitory potencies (BACE-1 IC50 50 ～1 μM).

2-OXAZOLIDINONES AND THEIR USE AS INHIBITORS OF ANIMAL CELL MOTILITY AND GROWTH

Cell motility and growth inhibitors, including compounds of the general structural formula (I), and use of the cell motility and cell growth inhibitors, and pharmaceutically acceptable salts, pro-drugs, and solvates thereof, as therapeutic agents, are disclosed.