Potassium Phosphate, Tribasic → HCID 58547240, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 3-(3-chloro-quinoxalin-2-yl)-azetidine-1-carboxylic acid tert-butyl ester (46) (639 mg, 2.0 mmol, as prepared in the above Preparation 14), 3-methyl-phenylboronic acid (68) (299.2 mg, 2.2 mmol), K3PO4 (818 mg, 4.0 mmol) in dioxane (20 mL) and water (4 mL) was added Pd(dppf)Cl2 (73.2 mg, 0.1 mmol) then the reaction mixture was stirred at 90° C. under nitrogen atmosphere overnight. The reaction mixture was filtered through CELITE® and washed with EtOAc (50 mL). The filtrate was concentrated and the crude product was purified by silica gel column to give 3-(3-m-tolyl-quinoxalin-2-yl)-azetidine-1-carboxylic acid tert-butyl ester (69) (637 mg, 1.7 mmol, yield 85%).

Provenance & Evidence