536746-99-3

Upstream product

• 76-83-5 trityl chloride 
• 114676-59-4 (2R,4R)-4-hydroxy-2-methoxycarbonylpyrrolidine hydrochloride 
• 79-06-1 2-propenamide 
• 62-53-3 aniline 
• 2584-71-6 cis-hydroxy-D-proline 

Downstream Products

• 133039-01-7 (3R,5R)-5-Hydroxymethyl-1-trityl-pyrrolidin-3-ol 
• 133039-00-6 (1R,4R)-5-Trityl-2-oxa-5-aza-bicyclo[2.2.1]heptan-3-ol 
• 1611487-95-6 (3S,5S)-(9H-fluoren-9-yl)methyl 3-amino-5-fluoropiperidine-1-carboxylate hydrochloride 
• 1611487-97-8 N-((3S,5S)-5-fluoropiperidin-3-yl)-4-nitrobenzamide 
• 1611487-98-9 N-((3S,5S)-5-fluoropiperidin-3-yl)-3-nitrobenzamide 
• 1611487-99-0 N-((3S,5S)-5-fluoropiperidin-3-yl)-2-nitrobenzamide 
• 1611480-96-6 tert-butyl (3S,5S)-1-benzoyl-5-fluoropiperidin-3-ylcarbamate 
• 1611481-03-8 tert-butyl (3S,5S)-5-fluoro-1-(4-methoxybenzoyl)piperidin-3-ylcarbamate 
• 1611480-90-0 tert-butyl (3S,5S)-5-fluoro-1-tritylpiperidin-3-ylcarbamate 
• 1593969-81-3 tert-butyl N-[(3S,5S)-5-fluoropiperidin-3-yl]carbamate 
• 1611480-97-7 ((3S,5S)-3-amino-5-fluoropiperidin-1-yl)(phenyl)methanone 
• 1611481-04-9 ((3S,5S)-3-amino-5-fluoropiperidin-1-yl)(4-methoxyphenyl)methanone 
• 1611481-05-0 ((3S,5S)-3-amino-5-fluoropiperidin-1-yl)(3-methoxyphenyl)methanone 
• 1611481-06-1 ((3S,5S)-3-amino-5-fluoropiperidin-1-yl)(2-methoxyphenyl)methanone 

Relevant academic research and scientific papers

Enantioselective synthesis and physicochemical properties of libraries of 3-amino- and 3-amidofluoropiperidines

The enantioselective syntheses of 3-amino-5-fluoropiperidines and 3-amino-5,5-difluoropiperidines were developed using the ring enlargement of prolinols to access libraries of 3-amino- and 3-amidofluoropiperidines. The study of the physicochemical properties revealed that fluorine atom(s) decrease(s) the pKa and modulate(s) the lipophilicity of 3-aminopiperidines. The relative stereochemistry of the fluorine atoms with the amino groups at C3 on the piperidine core has a small effect on the pK a due to conformationnal modifications induced by fluorine atom(s). In the protonated forms, the C-F bond is in an axial position due to a dipole-dipole interaction between the N-H+ and C-F bonds. Predictions of the physicochemical properties using common software appeared to be limited to determine correct values of pKa and/or differences of pK a between cis- and trans-3-amino-5-fluoropiperidines.

Access to optically active 3-azido- and 3-aminopiperidine derivatives by enantioselective ring expansion of prolinols

The activation of N-alkyl prolinols by XtalFluor E allowed the formation of an aziridinium intermediate that can react with tetrabutylammonium azide (nBu4NN3) to produce 3-azidopiperidines and/or 2-(azidomethyl)pyrrolidines, in a rat

N-HYDROXYAMIDE DERIVATIVES POSSESSING ANTIBACTERIAL ACTIVITY

Novel N-hydroxyamide derivatives are disclosed. These N-hydroxyamide derivatives inhibit UPD-3O-(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase, an enzyme present in gram negative bacteria and are therefore useful as antimicrobials and antibiotics. Methods of synthesis and of use of the compounds are also disclosed.

Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade

The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.