Potassium Phosphate, Tribasic → HCID 9981742, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of trifluoromethanesulfonic acid 2-[6-(quinolin-7-yloxy)-pyrimidin-4-yl]-5-trifluoromethylphenyl ester, (Example 192(a)), (100 mg, 0.19 mmol), 4-fluorophenyl boronic acid (41 mg, 0.29 mmol, Aldrich), K3PO4 (82 mg, 0.39 mmol), KBr (35 mg, 0.29 mmol) and Pd(PPh3)4 (11 mg, 0.010 mmol, Strem) in dioxane (2.0 mL) was stirred and heated by microwave synthesizer at 140° C. for 10 min. The mixture was partitioned between CH2Cl2 and 1 N NaOH. The organic phase was separated, and the aqueous phase was extracted with CH2Cl2. The combined extracts were dried over Na2SO4, filtered and concentrated in vacuum. Purification by silica gel chromatography (gradient 0.5 to 3.0 % MeOH/CH2Cl2) afforded the title compound as a white amorphous solid. MS (ESI, pos. ion) m/z: 462 (M+1).

Provenance & Evidence