Cyclopropylamine → {3-[3-(Cyclopropylamino)-1,2,4-oxadiazol-5-yl]-5-[4-(trifluoromethyl)phenyl]piperidin-1-yl}-(morpholin-4-yl)methanone

Participants

Reaction Steps

To a solution of 150 mg (0.337 mmol) of the oxadiazole from Example 23A in 1.5 ml of ethanol were added 385 mg (6.74 mmol) of cyclopropylamine, and then the reaction mixture was stirred in the microwave at 80 for 2 h. Another 385 mg (6.74 mmol) of cyclopropylamine were added and the mixture was stirred in the microwave at 80° C. for a further 2 h. This was followed by stirring in the microwave at 90° C. for 1 h. The solvent was removed under reduced pressure and the crude product was purified by means of preparative HPLC. Yield: 95.3 mg (61% of theory)

Provenance & Evidence