Potassium Phosphate, Tribasic → HCID 54671271, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 2-[1-(3-chloro-pyrazin-2-yl)-azetidin-3-yl]-quinoline, as prepared in the above Step 3 of Example 57, (150 mg, 0.51 mmol), 3-methyl-phenylboronic acid (75 mg, 0.51 mmol) and K3PO4 (211 mg, 1 mmol) in 1,4-dioxane (12 mL) and H2O (3 mL) was added Pd(dppf)Cl2 (35 mg, 0.05 mmol) then the reaction mixture was stirred at 110° C. under N2 overnight. The reaction mixture was filtered through CELITE™ and washed with CH2Cl2 (50 mL). The organic layer was concentrated and the crude product was purified by silica gel column to give 2-[1-(3-m-tolyl-pyrazin-2-yl)-azetidin-3-yl]-quinoline (50 mg, 0.14 mmol, yield 28%).

Provenance & Evidence