Lithium Hydroxide → 3-{4-[(E)-3-(3,4-Dichloro-phenyl)-acryloyl]-7-oxo-[1,4]diazepan-1-yl}-propionic acid

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Reaction Steps

A solution of 3.50 g (8.47 mmol) of 3-{4-[(E)-3-(3,4-dichloro-phenyl)-acryloyl]-7-oxo-[1,4]diazepan-1-yl}-propionic acid ethyl ester in 80 ml of tetrahydrofuran/ethanol (1:1) was treated at 0° C. with 16.94 ml (16.94 mmol) of 1 M aq. lithium hydroxide solution, and kept 3 h at this temperature. The reaction was neutralized with cold aqueous 10% KHSO4 and extracted with EtOAc (3×). The organic phases were washed with aqueous 10% NaCl, dried over Na2SO4 and evaporated to yield 3.20 g (98%) of the titled compound as white solid. MS: 385.0 (MH+, 2Cl).

Provenance & Evidence