95501-78-3

Upstream product

• 13734-41-3 t-Boc-L-valine 
• 87694-52-8 tert-butyl (S)-1-(N-methoxy-N-methylcarbamoyl)-2-methylpropylcarbamate 
• 2026-48-4 (S)-valinol 
• 72-18-4 L-valine 
• 143961-92-6 {(S)-1-[(S)-2-((S)-1-Hydroxymethyl-2-methyl-propylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-carbamic acid benzyl ester 
• 122-51-0 orthoformic acid triethyl ester 
• 1149-26-4 (S)-N-(benzyloxycarbonyl)valine 
• 71989-31-6 Fmoc-Pro-OH 
• 79069-51-5 (S)-N-tert-butoxycarbonylvalinal 

Downstream Products

• 1026319-41-4 [(S)-1-((S)-2-{(S)-1-[Hydroxy-((S)-4-methyl-4,5-dihydro-oxazol-2-yl)-methyl]-2-methyl-propylcarbamoyl}-pyrrolidine-1-carbonyl)-2-methyl-propyl]-carbamic acid benzyl ester 
• 1026813-21-7 ((S)-1-{(S)-2-[(S)-1-(Benzothiazol-2-yl-hydroxy-methyl)-2-methyl-propylcarbamoyl]-pyrrolidine-1-carbonyl}-2-methyl-propyl)-carbamic acid benzyl ester 
• 1026520-48-8 [(S)-1-((S)-2-{(S)-1-[(1H-Benzoimidazol-2-yl)-hydroxy-methyl]-2-methyl-propylcarbamoyl}-pyrrolidine-1-carbonyl)-2-methyl-propyl]-carbamic acid benzyl ester 
• 105108-37-0 {(S)-2-Methyl-1-[(S)-2-(3,3,3-trifluoro-2-hydroxy-1-isopropyl-propylcarbamoyl)-pyrrolidine-1-carbonyl]-propyl}-carbamic acid benzyl ester 
• 105080-60-2 {(S)-2-Methyl-1-[(S)-2-((S)-3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidine-1-carbonyl]-propyl}-carbamic acid benzyl ester 
• 120629-54-1 (1S)-Benzyloxycarbonyl-L-valyl-N-[3-ethoxy-2-hydroxy-3-imino-1-(1-methylethyl)propyl]-L-prolinamide hydrochloride 
• 120629-47-2 (benzyloxycarbonyl)-L-valyl-N-<1-<(2-benzoxazolyl)hydroxymethyl>-2-methylpropyl>-L-prolinamide 
• 138754-80-0 <(benzyloxycarbonyl)-L-valyl>-N-<1-<(2-benzoxazolyl)carbonyl>-2-methylpropyl>-L-prolinamide 
• 161443-20-5 (benzyloxycarbonyl)-L-valyl-N-<1-<(2-oxazolinyl)hydroxymethyl>-2-methylpropyl>-L-prolinamide 
• 138754-95-7 (benzyloxycarbonyl)-L-valyl-N-<1-<(2-oxazolinyl)carbonyl>-2-methylpropyl>-L-prolinamide 
• 138754-97-9 (S)-(benzyloxycarbonyl)-L-valyl-N-<1-acetyl-2-methylpropyl>-L-prolinamide 

Relevant academic research and scientific papers

A practical method for the combinatorial synthesis of peptide aldehydes

A practical strategy for solid phase synthesis of peptide aldehydes is described. An olefin linker is constructed using Wittig chemistry, after peptide synthesis ozonolytic treatment of the linker and subsequent workup with dimethyl sulphide results in fa

A Method For The Stereoselective Synthesis of Peptidyl Trifluoromethyl Ketones

A method is described for the stereoselective preparation of peptidyl trifluoromethyl ketones which is centered around the addition of trifluoromethyl zinc iodide to a peptidyl aldehyde.Oxidation of the resulting alcohol with selected oxidants affords the corresponding ketone in greater than 99percent isomeric purity.

SELECTED DIFLUORO DERIVATIVES

The invention discloses a series of difluoroketone, mono-di-and tri-peptide derivatives of formula Ia, Ib and Ic: ______________________________________ (Formula set out on pages following Examples) Ia (Formula set out on pages following Examples) Ib (Formula set out on pages following Examples) Ic ______________________________________ and salts thereof where appropriate, and wherein the radicals are defined hereafter in the specification. The derivatives are useful in inhibiting the action of human leukocyte elastase. There are also disclosed methods and intermediates for the manufacture of, and pharmaceutical compositions comprising, the said derivatives.

PROLINE DERIVATIVES

Proline derivatives of the formulae: STR1 wherein R 1 through R 11 have defined values, and acid-and base-addition salts thereof, and equilibrium addition compounds of the aldehyde group thereof; processes for their preparation; pharmaceutical compositions; and intermediates for preparing said proline derivatives. The proline derivatives are human leukocyte elastase inhibitors which are useful, for example, in treating pulmonary emphysema.