Reaction #1888

Reaction equation

trans-7-chloro-5-(2-chlorophenyl)-1-isobutyl-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepine-3-acetic acid

ammonium chloride

1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride

triethylamine

→

crystal

Yield 75.2%

Trans-7-chloro-5-(2-chlorophenyl)-1-isobutyl-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepine-3-acetamide

Yield 75.2%

Solvents

dimethylformamide

water

Conditions

Workup

1. 1
   workup.ADDITIONwere added
2. 2
   Extractionthe solution was extracted with ethyl acetate
3. 3
   Washby washing with water
4. 4
   Otherafter which the solvent was removed
5. 5
   Otherthe residue was recrystallized

Procedure

1.0 g of trans-7-chloro-5-(2-chlorophenyl)-1-isobutyl-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepine-3-acetic acid and 0.5 g of ammonium chloride were dissolved in 8 mi of dimethylformamide, and 0.46 g of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride and 0.7 ml of triethylamine were added, followed by stirring at room temperature for 30 minutes. After water was added, the solution was extracted with ethyl acetate, followed by washing with water, after which the solvent was removed and the residue was recrystallized to yield 0.75 g of a crystal.

Source