1434818-59-3

Upstream product

• 87250-97-3 2’-methyl-2’-propanyl (1S,4S)-3-oxo-2-oxa-5-azabicyclo[2.2.1]heptane-5-carboxylate 
• 1434816-31-5 (2S,4S)-4-hydroxy-1-(1-trifluoromethylcyclopropanecarbonyl)pyrrolidine-2-carboxylic acid (1-cyanocyclopropyl)amide 
• 1434816-61-1 (2S,4R)-4-methanesulfonyloxy-1-(1-trifluoromethyl-cyclopropanecarbonyl)-pyrrolidine-2-carboxylic acid methyl ester 
• 1434816-48-4 (1S,4S)-5-(1-trifluoromethyl-cyclopropanecarbonyl)-2-oxa-5-aza-bicyclo[2.2.1]heptan-3-one 
• 848074-36-2 1-(trifluoromethyl)cyclopropanecarbonyl chloride 
• 277756-46-4 1-(trifluoromethyl)cyclopropanecarboxylic acid 
• 1434817-67-0 4-(2-methyl-pyridin-4-yl)-2-trifluoromethylbenzenethiol hydrochloride 
• 1434818-87-7 methanesulfonic acid (3S,5S)-5-(1-cyano-cyclopropylcarbamoyl)-1-(1-trifluoromethyl-cyclopropanecarbonyl)-pyrrolidin-3-yl ester 
• 1434817-47-6 3-(4-bromo-2-trifluoromethyl-phenylsulfanyl)propionamide 
• 1208075-10-8 4-bromo-2-(trifluoromethyl)benzenethiol 
• 176225-10-8 4-bromo-2-(trifluoromethyl)benzene-1-sulfonyl chloride 
• 1434817-41-0 3-[4-(2-methylpyridin-4-yl)-2-trifluoromethylphenylsulfanyl]propionamide 
• 1434818-13-9 benzenesulfonic acid (3S,5S)-5-(1-cyano-cyclopropylcarbamoyl)-1-(1-trifluoromethylcyclopropanecarbonyl)-pyrrolidin-3-yl ester 

Downstream Products

• 1252637-46-9 (2S,4R)-4-[4-(2-methylpyridin-4-yl)-2-trifluoromethylbenzenesulfonyl]-1-(1-trifluoromethylcyclopropanecarbonyl)pyrrolidine-2-carboxylic acid (1-cyanocyclopropyl)amide 

Relevant academic research and scientific papers

PROCESS FOR THE PREPARATION OF PROLINE DERIVATIVES

The present invention relates in part to a process for the preparation of a proline derivative of formula I wherein, R1 is C1-7-alkyl or wherein R4 is selected from the group consisting of C1-7-alkyl, halogen-C1-7-alkyl and phenyl optionally substituted by halogen; R2 is halogen or halogen-C1-7-alkyl; and R3 is selected from the group consisting of hydrogen, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, halogen-C1-7-alkoxy and a 5- or 6-membered heterocyclic ring containing one or two nitrogen atoms, said ring being optionally substituted by C1-7-alkyl or halogen. The proline derivatives of the formula I are preferential inhibitors of the cysteine protease Cathepsin S and are therefore useful to treat metabolic diseases like diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral arterial disease and diabetic nephropathy.