1-((4-Chlorophenyl)methyl)piperidin-4-amine → N-(2-{(2R)-3-[1-(4-Chloro-benzyl)-piperidin-4-ylamino]-2-hydroxy-2-methylpropoxy}-phenyl)-acetamide

Participants

Reaction Steps

1-(4-chlorobenzyl)-4-piperidinamine (62 mg, 0.276 mmol) and N-(2-{[(2R)-2-methyloxiranyl]methoxy}phenyl)acetamide (61 mg, 0.276 mmol) in ethanol (1.5 ml) was stirred in a sealed vial at 80° C. for 4 hours. The reaction mixture was diluted with water and purified by reversed phase HPLC to give 130 mg (70%) of the title compound as a ditrifluoroacetate after lyophilisation. The optical purity was determined to 86% ee, by chiral HPLC on a Chiralpak AD-column.

Provenance & Evidence