1,8-Diazabicyclo(5.4.0)undec-7-ene → N-[3-Chloro-4-(trifluoromethyl)phenyl]-4-{[(3S)-1-cyclopropylpiperidin-3-yl]methyl}piperazine-1-carboxamide

Participants

Reaction Conditions

Reaction Steps

A mixture of 1-{[(3S)-1-cyclopropylpiperidin-3-yl]methyl}piperazine (67 mg), 2,2,2-trichloro-N-[3-chloro-4-(trifluoromethyl)phenyl]acetamide (102 mg) and DBU (46 mg) in acetonitrile (4 mL) was heated to 150° C. in the microwave for 10 minutes. The solution was concentrated at reduced pressure and purified by reverse phase prep HPLC eluting with a mixture of 5-95% acetonitrile in water and then SCX-2 column eluting with methanol then 7M NH3 in methanol to give the title compound as a white solid (55 mg, 41%).

Provenance & Evidence