1-Hydroxybenzotriazole → HCID 67140010, compound

Participants

Reaction Steps

To a solution of the title I compound, 2-(2-amino-benzoylamino)-3-(3-benzyloxy-4-nitro-phenyl)-propionic acid (317 mg, 0.728 mmol) in CH2Cl2 (10 mL) is added HOBt (111.5 mg, 0.728 mmol) and 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDAC.HCl, 140 mg, 0,72 mmol) and the mixture is stirred at RT for 4 h and evaporated. The residue is partitioned between EtOAc and water and the organic solution is washed with 1N aqueous HCl, water, saturated aqueous NaHCO3 and brine, dried over anhydrous MgSO4, decolorized and evaporated to a small volume. The precipitated product is collected by filtration and dried to give 3-(3-benzyloxy-4-nitro-benzyl)-3,4-dihydro-1H-benzo[1,4]diazepine-2,5-dione: mp=243-245° C.

Provenance & Evidence