Hydrochloric Acid → HCID 68183134, compound

Participants

Reaction Steps

To a mixture of 3-[amino(4-chlorophenyl)methyl]-4-cyano-5-(morpholin-4-yl)thiophene-2-carboxylic acid.HCl (0.206 g, 0.497 mmol), 1-Hydroxybenzotriazole hydrate (92.1 mg, 0.601 mmol) and N-(3-Dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (188 mg, 0.981 mmol) in dry Methylene chloride (10.0 mL, 156 mmol) was added N,N-Diisopropylethylamine (0.252 mL, 1.45 mmol). The resulted clear solution was stirred at r.t. for 21 hours. The reaction solution was diluted with DCM (−30 mL), washed with water (3×), brine, dried over anhydrous Na2SO4, filtered and rotavaped to give a crude product. Chromatograph in a silica gel column using MeOH/DCM (0/100 to 3/97) afforded a racemic product (0.138 g, yield 74.8%).

Provenance & Evidence