Hydrochloric Acid → Elinzanetant

Participants

Reaction Steps

2-[3,5-bis(trifluoromethyl)phenyl]-N-[6-[(7S,9aS)-7-({[(1,1-dimethylethyl)(dimethyl)silyl]oxy}methyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-4-(4-fluoro-2-methylphenyl)-3-pyridinyl]-N,2-dimethylpropanamide (D24) (390 mg, 0.498 mmol) was dissolved 17 mL of methanol. To this solution was added concentrated HCl (0.9 mL) at 0° C., and stirring was continued at room temperature for 3 h (complete conversion). The reaction mixture was loaded on a SCX cartridge and washed with MeOH. The product was eluted with 0.5 M methanolic ammonia. The product-containing fractions were evaporated, leaving the target compound as a white solid: 310 mg, 0.464 mmol, 93%.

Provenance & Evidence