107600-13-5

Upstream product

• 76-83-5 trityl chloride 
• 100841-17-6 4-methyl-2(S)-<(triphenylmethyl)amino>-1-pentanol 

Downstream Products

• 107600-09-9 {(S)-1-[(S)-1-((1S,2R,3R,4R)-2,3-Dihydroxy-1-isobutyl-5-methyl-4-{(1S,2S)-2-methyl-1-[(pyridin-2-ylmethyl)-carbamoyl]-butylcarbamoyl}-hexylcarbamoyl)-2-(3H-imidazol-4-yl)-ethylcarbamoyl]-2-phenyl-ethyl}-carbamic acid tert-butyl ester 
• 107600-10-2 <5(S)-<<-L-histidyl>amino>-3(R),4(R)-dihydroxy-2(R)-isopropyl-7-methyloctanoyl>-2(S)-methylbutylamine 
• 107600-00-0 3-<3(R)-<3-(tert-butyloxycarbonyl)-2,2-dimethyl-4(S)-isobutyl-5(R)-oxazolidinyl>-3-hydroxy-2(R)-isopropyl-1-oxopropyl>-4(R)-methyl-5(S)-phenyl-2-oxazolidinone 
• 132065-47-5 (2RS,4S,5RS)-4-isobutyl-2-phenylselenanylmethyl-3-(p-tolylsulfonyl)-5-vinyloxazolidine 
• 132065-40-8 (2RS,4S,5RS)-3-benzyloxycarbonyl-4-isobutyl-2-phenylselenanylmethyl-5-vinyloxazolidine 
• 132065-42-0 (7S)-1-benzyloxycarbonyl-7-isobutyl-1,3,4,7-tetrahydroazepin-2-one 
• 132065-46-4 (3RS,4S)-6-methyl-4-(p-tolylsulfonylamino)hept-1-en-3-ol 
• 123802-17-5 (3RS,4S)-4-benzyloxycarbonylamino-6-methylhept-1-en-3-ol 
• 330817-14-6 (3R,4S)-6-Methyl-2-methylene-4-(trityl-amino)-heptane-1,3-diol 
• 330817-15-7 (3S,4S)-6-Methyl-2-methylene-4-(trityl-amino)-heptane-1,3-diol 
• 123381-26-0 (2S,3S)-dimethyl <2-hydroxy-5-methyl-3-(tritylamino)hexyl>phosphonate 
• 123381-25-9 (2R,3S)-dimethyl <2-hydroxy-5-methyl-3-(tritylamino)hexyl>phosphonate 
• 153451-35-5 N-trityl-3-methyl-1-vinyl-butylamine 

Relevant academic research and scientific papers

New Synthetic Methodology for the Synthesis of 7-Substituted Tetrahydroazepin-2-ones

The Claisen rearrangement of the vinyl substituted ketene aminals 2 (R = CH2CHMe2, CH2OSit-BuMe2) which were generated in situ by selenoxide elimination of the aminal precursors 3 in the presence of 1,8-diazabicycloundec-7-ene (DBU) furnished the enantiomerically pure 7-substituted tetrahydroazepin-2-ones 1.

New inhibitors of renin that contain novel phosphostatine Leu-Val replacements

A novel series of renin inhibitors based on the Phe8-His9-Leu10-Val11 substructure of renin's natural substrate, angiotensinogen, is reported. These inhibitors retain the Phe8-His9 portion of the native substructure and employ novel phosphostatine Leu10-Val11 replacements (LVRs). The phosphostatine LVRs were prepared by condensing a dialkyl phosphonate ester stabilized anion with either N-t-Boc-amino aldehydes or N-tritylamino aldehydes (derived from the corresponding amino acid). Structure-activity relationships at the Leu10 side chain revealed that the LVR derived from L-cyclohexylalanine provided a 130-fold boost in potency over the LVR derived from L-leucine. The dialkyl ester moiety was varied and a loss in potency was incurred when the alkyl ester was chain extended or α-branced; dimethyl esters provided optimum potency. The phosphonate moiety was replaced by a half-acid half-ester phosphonate and dimethylphosphinate; both replacements lead to a loss in potency. The more potent inhibitors (IC50 = 20-50 nM) were found to be selective inhibitors for renin over porcine pepsin and bovine cathepsin D (little or no inhibition was observed at 10-5 M).

Renin Inhibitors. Design of Angiotensinogen Transition-State Analogues Containing Novel (2R,3R,4R,5S)-5-Amino-3,4-dihydroxy-2-isopropyl-7-methyloctanoic Acid

A highly stereoselective synthesis of 2(R)--3-methylbutyl>-2,2-dimethyl-4(R)-dioxolanyl>-3-methylbutanoic acid (11) is described.This is a suitably protected carboxylic acid useful as an intermediate for the prepa