Cyclohexanecarboxylic acid → 1-Cyclobutyl-4-{[1-(cyclohexylcarbonyl)azetidin-3-yl]carbonyl}-1,4-diazepane

Participants

Reaction Steps

To a stirred solution of cyclohexanecarboxylic acid (10.8 mg, 0.084 mmol) in DCM/DMF (1.1 ml) was added HOBt (11.4 mg, 0.084 mmol) and EDCI (16.1 mg, 0.084 mmol). After 10 mins a solution of 1-(azetidin-3-ylcarbonyl)-4-cyclobutyl-1,4-diazepane (20 mg, 0.084 mmol) in DCM (1 ml) and DIPEA (0.01 ml, 0.084 mmol) was added dropwise. After 15 h the solvent was evaporated at reduced pressure and purified by silica FCC (eluting with 99:1 to 95:5 gradient of DCM/2M NH3 in MeOH) to give the title compound (24 mg, 82% yield) as brown oil.

Provenance & Evidence