115654-51-8

Upstream product

• 7722-84-1 dihydrogen peroxide 
• 280-64-8 9-bora-bicyclo[3.3.1]nonane 
• 104856-06-6 tert-butyl [(1S,2S)-1-(cyclohexylmethyl)-2-hydroxy-3-butenyl]carbamate 
• 104856-08-8 (4S,5S)-4-(cyclohexylmethyl)-5-vinyloxazolidin-2-one 
• 104856-09-9 (3S,4S)-4-amino-5-cyclohexyl-3-hydroxy-1-pentene 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 122079-09-8 (2S,3S)-2-Amino-5-azido-1-cyclohexyl-pentan-3-ol 

Relevant academic research and scientific papers

Azido Glycols: Potent, Low Molecular Weight Renin Inhibitors Containing an Unusual Post Scissile Site Residue

Azidomethyl-substituted 1,2- and 1,3-diols were prepared from Boc-cyclohexylalanal and evaluated as transition state analogue renin inhibitors, leading to the development of a small (MW 600), nanomolar inhibitor.Remarkable aqueous solubility enhancement followed the incorporation of an N-terminal urea functionality.Evaluation of selected compounds both in vivo and in vitro demonstrated that while transport across the intestine occurred upon id administration, extensive liver extraction resulted in low systemic levels.

Angiotensinogen analogs

The invention relates to renin inhibiting compounds of the formula STR1 wherein A is hydrogen; loweralkyl; arylalkyl; OR10 or SR10 wherein R10 is hydrogen, loweralkyl or aminoalkyl; NR11 R12 wherein R11 and R12 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; STR2 wherein B is NH, alkylamino, S, O, CH2 or CHOH and R13 is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, aminoalkyl, alkoxycarbonylalkyl, carboxyalkyl, N-protected aminoalkyl, alkylaminoalkyl, (N-protected)(alkyl)aminoalkyl, dialkylaminoalkyl, (heterocyclic) alkyl or a substituted or unsubstituted heterocyclic; W is CO or CHOH and U is CH2 or NR2 with the proviso that when W is CHOH then U is CH2 ; R1 is loweralkyl, cycloaklylmethyl, benzyl, α,α-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)-methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R1 is phenoxy, thiophenoxy or anilino, B is CH2 or CHOH or A is hydrogen, R3 is loweralkyl, vinylloweralkyl, benzyl or heterocyclic ring substituted methyl, R5 is loweralkyl, cycloalkylmethyl or benzyl; R2 and R4 are independently selected from hydrogen and loweralkyl; R6 is CHOH or CO; R7 is CH2, CF2 or CF with the proviso that when R6 is CO, R7 is CF2 ; R8 is CH2, CHR14 wherein R14 is lower-alkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, or R7 and R8 taken together can be STR3 with the proviso that when R7 is CF2, R8 is CH2 ; E is O, S, SO, SO2, NR15 wherein R15 is hydrogen or loweralkyl or NR16 CO wherein R16 is hydrogen or loweralkyl; R9 is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protected group, or E and R9 taken together can be N3, with the proviso that when E is NH, R9 is an N-protecting group; and pharmaceutically acceptable salts thereof.