106942-45-4

Upstream product

• 28897-81-6 2-phenyl-4-iso-propyl-4H-oxazolin-5-one 
• 2901-80-6 N-benzoyl-D,L-valine 
• 98-88-4 benzoyl chloride 
• 106942-36-3 4-Isopropyl-2-phenyl-4-(2,2,2-trifluoro-acetyl)-4H-oxazol-5-one 

Downstream Products

• 106746-07-0 N-(3,3,3-trifluoro-2-hydroxy-1-(methylethyl)propyl)benzamide 
• 106771-22-6 N-<<5-(dimethylamino)-1-naphtalenyl>sulfonyl>-L-alanyl-L-alanyl-N-<3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl>-L-prolinamide 
• 123206-21-3 D-phenylalanyl-N-<3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl>-L-prolinamide hydrochloride 
• 123206-19-9 N-(4-methoxy-1,4-dioxobutyl)-L-alanyl-L-alanyl-N-<3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl>-L-prolinamide 
• 123206-22-4 N-(4-methoxy-1,4-dioxobutyl)-D-phenylalanyl-N-<3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl>-L-prolinamide 
• 123206-20-2 N-<(1,1-dimethylethoxy)carbonyl>-D-phenylalanyl-N-<3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl>-L-prolinamide 
• 123239-02-1 N-<(1,1-dimethylethoxy)carbonyl>-D-phenylalanyl-N-<3,3,3-trifluoro-2-hydroxy-1-(1-methylethyl)propyl>-L-prolinamide 
• 106746-09-2 3(RS)-amino-1,1,1-trifluoro-2(RS)-hydroxy-4-methylpentane hydrochloride 

Relevant academic research and scientific papers

Base-catalysed 18F-labelling of trifluoromethyl ketones. Application to the synthesis of 18F-labelled neutrophil elastase inhibitors

A new method for the fluorine-18 labelling of trifluoromethyl ketones has been developed. This method is based on the conversion of a-COCF3 functional group to a difluoro enol silyl ether followed by halogenation and fluorine-18 labelling. The utility of this new method was demonstrated by the synthesis of fluorine-18 labelled neutrophil elastase inhibitors, which are potentially useful for detection of inflammatory disorders.

Synthesis of peptidyl fluoromethyl ketones and peptidyl α-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, and rat and human neutrophil cathepsin G

Comparison of MeO-Suc-Val-Pro-Phe-CO2Me (29) and MeO-Suc-Ala-Ala-Pro-Phe-CO2Me (25) with their corresponding trifluoromethyl ketones 9a and 9b, respectively, in rat and human neutrophil cathepsin G assays showed the α-keto esters to

SYNTHESIS OF FLUORINATED α-AMINO KETONES PART I: α-BENZAMIDOALKYL MONO- DI- AND TRIFLUOROMETHYL KETONES

2-Phenyl-5(4H)-oxazolones, obtained from α-amino acids, are reacted with di- and trifluoro acetic anhydride by a modified Dakin-West procedure to yield in a one-pot reaction α-benzamidoalkyl-di- and trifluoromethyl ketones in good yields.The monofluoromethyl analogues were also prepared from α-amino acids, however the use of the highly toxic fluoroacetic anhydride was avoided.The key step is the halogen exchange reaction on the corresponding bromomethyl ketone.