1-Hydroxybenzotriazole → 4-(2-Oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-[1-(3,4-diethyl-benzyl)-2-(1'-methyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl]-amide

Participants

Reaction Conditions

Reaction Steps

0.3 mL of triethylamine, 323 mg (1.01 mmol) of TBTU, 155 mg (1.01 mmol) of HOBt and 184 mg (1.01 mmol) of methyl-[4,4′]bipiperidinyl were added to a solution of 500 mg (1.02 mmol) of 3-(3,4-diethyl-phenyl)-2-{[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carbonyl]-amino}-propionic acid in 50 mL of THF and stirred for 4 h at RT and 2 h at 40° C. The reaction mixture was evaporated down, the residue was stirred with 40 mL of saturated NaHCO3 solution, the precipitated product was suction filtered, washed twice with water and triturated with EtOH. The white substance precipitated was suction filtered and washed twice with diethyl ether.

Provenance & Evidence