(R)-3-Pyrrolidinol → 3-(4-Ethylphenyl)-5-{3-[(3R)-3-hydroxypyrrolidin-1-yl]-1,2,4-oxadiazol-5-yl}piperidin-1-yl(4-hydroxypiperidin-1-yl)methanone

Participants

Reaction Steps

To a solution of 80.0 mg (0.191 mmol) of the oxadiazole from Example 25A in 1.20 ml of ethanol were added 333 mg (3.82 mmol) of (3R)-pyrrolidin-3-ol, and then the reaction mixture was stirred in the microwave at 80 for 2 h. The solvent was removed under reduced pressure, dichloromethane was added and the mixture was washed with water. The organic phase was dried over magnesium sulphate, filtered and concentrated under reduced pressure. Yield: 64.8 mg (70% of theory)

Provenance & Evidence