Hydrochloric Acid → Delapril Hydrochloride

Participants

Reaction Steps

To tert-butyl N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-(S)-alanyl-N-(2-indanyl)glycinate (1.4 g, 2.75 mmoles) was added p-dioxane which had been saturated with anhydrous hydrogen chloride (35 ml). the resulting solution was stirred for two and a half hourst at room temperature and then solvent was evaporated to afford a colorless solid. Anhydrous diethyl ether was added to the residue and the product was filtered and washed with a small amount of ether to give N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-(S)-alanyl-N-(2-indanyl)glycine hydrochloride (1.1 g, 84.6%) as a colorless solid: m.p. 181°; [α]DETOH=+16.44°; mass spectra (CI): 435.6(m+1-H2O, 100%).

Provenance & Evidence