Potassium Phosphate, Tribasic → HCID 57709058, compound

Participants

Reaction Conditions

Reaction Steps

A solution of palladium acetate (2.0 mg, 0.009 mmol), 2-dicyclohexylphosphino-2′,6′-dimethoxybiphenyl (7.4 mg, 0.018 mmol) and potassium phosphate (38.4 mg, 0.181 mmol) in water (0.032 mL) and toluene (0.150 mL) was stirred for three minutes. A solution of (4-chloro-2-fluoro-phenyl)acetic acid methyl ester (Example 40; 19.6 mg, 0.097 mmol) and 2-(4-{1-ethyl-1-[3-methyl-4-(1-trimethylsilanyloxy-cyclohexylethynyl)-phenyl]-propyl}-2-methyl-phenyl)-4,4,5,5-tetramethyl-[1,3,2]dioxaborolane (Example 35-(4); 37.1 mg, 0.0647 mmol) in toluene (0.18 mL) was added, and the mixture was stirred in a nitrogen atmosphere at 100° C. for one hour. After filtration through cotton plug, the filtrate was concentrated under reduced pressure. The residue was purified by thin layer silica gel chromatography (3% ethyl acetate/hexane) to give the title compound (30.9 mg, 77%).

Provenance & Evidence