Hydrochloric Acid → HCID 136451803, compound

Participants

Reaction Steps

A mixture of N-[(3RS)-1-(2-ethoxycabonylmethoxyphenyl)-carbonylmethyl-2,3-dihydro-5-(2-fluorophenyl)-9-methyl-2-oxo-1H-1,4-benzodiazepin-3-yl]-N′-{3-[1-(triphenylmethyl)tetrazol-5-yl]phenyl}urea (196 mg) and 1N NaOH in 1,2-dimethoxyethane (2 ml) was stirred at room temperature overnight. 4N-HCl in ethyl acetate (2 ml) was added to the reaction mixture and stirred at room temperature for three days. Ethyl acetate and water were added to the reaction mixture. The separated organic layer was washed with water and brine successively, and dried over magnesium sulfate. Removal of the solvent in vacuo afforded N-[(3RS)-2,3-dihydro-5-(2-fluorophenyl)-1-(2-carboxymethoxyphenyl)-carbonylmethyl-9-methyl-2-oxo-1H-1,4-benzodiazepin-3-yl]-N′-[3-(tetrazol-5-yl)phenyl]urea (66.0 mg, 47.4%).

Provenance & Evidence