Water → HCID 59536367, compound

Participants

Reaction Steps

1-(3-fluoro-4-(trifluoromethyl)phenyl)-1,2,3,4-tetrahydroisoquinoline (0.1500 g, 0.508 mmol, Example 71 Step 3) was dissolved in 3 mL CH2Cl2 and DIEA (0.0884 mL, 0.508 mmol) and 3-pyridyl isocyanate (0.0732 g, 0.610 mmol) were added at RT. The mixture was stirred over night and hydrolyzed with 2 mL water. The reaction was extracted 3 times with EtOAc (3×20 mL), dried over MgSO4 and evaporated. The crude product was purified via glass column chromatography providing 1-(3-fluoro-4-(trifluoromethyl)phenyl)-N-(pyridin-3-yl)-3,4-dihydroisoquinoline-2(1H)-carboxamide as a white solid. MS (ESI, positive ion) m/z: 416.0 (M+H). The majority of the material was submitted for chiral purification (SFC):

Provenance & Evidence