Triethylamine → 4-[4-(3-Chloro-4-trifluoromethoxy-phenyl)-7-oxo-[1,4]diazepan-1-yl]-butyric acid methyl ester

Participants

Reaction Steps

A solution of 0.16 g (0.3 mmol) of 4-{2-[(2-carboxy-ethyl)-(3-chloro-4-trifluoromethoxy-phenyl)-amino]-ethylamino}-butyric acid methyl ester dihydrochloride in 2.5 ml CH2Cl2 was treated with 0.04 ml (0.3 mmol) of triethylamine and at 0° C. with 0.08 g (0.4 mmol) of EDCI. The cooling bath was allowed to come to RT and after 15 h the reaction was extracted with aqueous 10% KHSO4/Et2O (3×). The organic phases were washed with 10% KHSO4, 10% NaCl and dried over Na2SO4 to yield after evaporation of the solvent 0.11 g (76%) of the title compound as a yellow oil. MS: 409.11 (MH+, Cl).

Provenance & Evidence