Hydrochloric Acid → 4-[(3-chloro-benzyl)-((R)-2-methyl-azetidine-2-carbonyl)-amino]-butyric acid methyl ester hydrochloride

Participants

Reaction Conditions

Reaction Steps

To a solution of (R)-2-[(3-chloro-benzyl)-(3-methoxycarbonyl-propyl)-carbamoyl]-2-methyl-azetidine-1-carboxylic acid tert-butyl ester, Intermediate 175 (17.6 g, 1 eq.) in 200 mL of dioxane under nitrogen was added a solution of HCl (4N) in dioxane (50 mL, 5 eq.). The reaction was stirred for 16 h at 20° C., then concentrated under reduced pressure. The crude was solubilised in DCM, poured into Et2O and the resulting solid was filtered, washed with Et2O and pentane and dried to afford 4-[(3-chloro-benzyl)-((R)-2-methyl-azetidine-2-carbonyl)-amino]-butyric acid methyl ester hydrochloride (12.5 g, yield=81%).

Provenance & Evidence