HCID 178418361, compound → HCID 178464362, compound

Participants

Reaction Steps

Under nitrogen atmosphere, a solution of (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid benzyl ester (7) (34.2 g, 37.88 mmol, >99% ee) obtained in Step 5 in ethanol (340 mL) was added with 10% Pd—C (wet, 3.4 for hydrogen substitution, and then the mixture was stirred at room temperature for 2 hours. The reaction suspension was filtered through Celite, and washed with ethanol (50 mL), and the washing solution was concentrated under reduced pressure to obtain substantially optically pure trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid (III) (white amorphous, 31.78 g, yield: 100%).

Provenance & Evidence