Hydrochloric Acid → HCID 67061903, compound

Participants

Reaction Steps

To a CH2Cl2 solution (0.05 M) of trans-tert-butyl 3-[(cyclopropyl{[5-(3-methoxypropyl)biphenyl-3-yl]methyl}amino)carbonyl]-4-(1-methyl-2-oxo-1,2-dihydropyridin-4-yl)piperidine-1-carboxylate (1 eq.) from the previous step was added HCl (4.0 M dioxane solution, 30 eq.). The resulting solution was stirred at RT for 45 min. Following the removal of the volatiles in vacuo, the resulting residue was directly loaded onto a SiO2 column packed with 93:7 (v/v) CH2Cl2:2.0 M NH3 in MeOH. Elution with the same solvent system furnished the title compound as a white froth. MS (ESI+, M+H): 514. Human Renin IC50 (buffer): 15 nM. Human Renin IC50 (plasma): 81 nM.

Provenance & Evidence