Reaction #165

ord-59518020213f4a99980578b9463ad852

Reaction equation

FC(F)(F)c1cnc(Cl)cc1I
FC(F)(F)c1cnc(Cl)cc1
CNC(=O)c1ccccc1N
CNC(=O)c1ccccc1N
CNC(=O)c1ccccc1Nc1cc(Cl)ncc1C(F)(F)F
CNC(=O)c1ccccc1Nc1cc
Yield 63.4%

Solvents

Conditions

Temperature
90°CELSIUS

Procedure

2-chloro-4-iodo-5-(trifluoromethyl)pyridine (500 mg, 1.63 mmol), 2-amino-N- methylbenzamide (244 mg, 1.63 mmol), diacetoxypalladium (29.2 mg, 0.13 mmol), (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (151 mg, 0.26 mmol) and cesium carbonate (636 mg, 1.95 mmol) were mixed together in dioxane (10 mL). Reaction was degassed with nitrogen and was stirred at 90 °C overnight under nitrogen. Reaction was filtered, washed with CH2Cl2 and filtrate was concentrated to dryness. The crude product was purified by flash chromatography on silica gel eluting with 10 to 50% ethyl acetate in petroleum ether. The solvent was evaporated to dryness to afford 2-(2-chloro-5-(trifluoromethyl)pyridin-4-ylamino)-N-methylbenzamide (340 mg, 63.4 %) as a pale yellow solid.

Source

750 AstraZeneca ELN dataset