Cesium carbonate → HCID 67247975, compound

Participants

Reaction Conditions

Reaction Steps

A stirred mixture of 7-acetyl-5-chloroquinolin-8-yl trifluoromethanesulfonate (0.17 g, 0.25 mmol, from Example 47, Step 2), N-piperidin-4-ylacetamide hydrochloride (0.040 g, 0.22 mmol), palladium acetate (1.0 mg, 0.0045 mmol), (S)-(−)-2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (4.2 mg, 0.0067 mmol), and cesium carbonate (0.28 g, 0.85 mmol) in tetrahydrofuran (4 mL) was heated at 65° C. overnight. The mixture was cooled, diluted with dichloromethane and filtered. The filtrate was washed with brine, dried over MgSO4, evaporated and purified on silica gel (eluting with 0 to 5% MeOH in dichloromethane) to give the desired product (42 mg, 54%). LCMS calculated for C18H21ClN3O2 (M+H)+: m/z=346.1; Found: 346.1.

Provenance & Evidence