Toluene → HCID 66680851, compound

Participants

Reaction Conditions

Reaction Steps

Under an Ar atmosphere, 10 mL of toluene, 2.5 mL of methanol, and 2.5 mL of 2M aqueous sodium carbonate solution were added to 500 mg (1.36 mmol) of methyl 2-{[(3-bromophenyl)carbonyl]amino}-5-chlorobenzoate obtained in Example 8-(i) and 352 mg (2.03 mmol) of isoquinolin-4-ylboronic acid, and the mixture was degassed. Further, 100 mg (0.087 mmol) of tetrakis(triphenylphosphine)palladium(0) was added, and the mixture was heated under stirring at 90° C. for 7 hours. The mixture was cooled to room temperature, and then water and ethyl acetate were added, followed by collection by filtration, water-washing, and drying. Thereafter, the resultant was dissolved in chloroform and filtered. The filtrate was condensed, thereby giving 360 mg of methyl 5-chloro-2-({[3-(isoquinolin-4-yl)phenyl]carbonyl}amino)benzoate (yield: 63%).

Provenance & Evidence