Dimethylformamide → Ethyl 3-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-{[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonyl]-amino}-propionate

Participants

Reaction Conditions

Reaction Steps

4.15 g (23.04 mmol) of CDT were added at 0° C. to a suspension of 8.00 g (23.04 mmol) of ethyl 2-amino-3-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-propionate and 16.0 mL (115.00 mmol) of triethylamine in 100 mL of DMF and the mixture was stirred for 1.5 h at 0° C. A solution of 5.64 g (23.00 mmol) of 3-piperidin-4-yl-1,3,4,5-tetrahydro-1,3-benzodiazepin-2-one in 200 mL of DMF was added and the mixture was heated to 100° C. for 2 h. The reaction mixture was cooled to RT, diluted with 1.5 L water and stirred for a further 10 min. The precipitate formed was filtered off, washed with water and dried i. vac.

Provenance & Evidence