A 2 L flask was charged with 35.0 g (175.8 mmol) of 2,4-dichloroquinoline,22.5 g (184.6 mmol) of phenylboronic acid, 6.1 g (5.3 mmol) of tetrakis(triphenylphosphine)palladium(0) were added to 800 mL of tetrahydrofuran and 400 mL of water, and the mixture was heated to 60 ?? C for 12 hours under a nitrogen stream. . The resulting mixture was added to methanol (3000 mL), and the crystallized solid was filtered and dissolved in toluene, filtered through silica gel / celite, and the organic solvent was removed in an appropriate amount, and then recrystallization from methanol gave Intermediate I-A52-1 (36.8 g, 87% yield).
