6-Methoxy-5-(4-methyl-1H-imidazol-1-YL)pyridin-2-amine → (R)-N-(6-methoxy-5-(4-methyl-1H-imidazol-1-yl)pyridin-2-yl)-4-methyl-2-phenyl-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepin-8-amine

Participants

Reaction Conditions

Reaction Steps

A solution of (R)-8-chloro-4-methyl-2-phenyl-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepine (83 mg, 0.30 mmol) and 6-methoxy-5-(4-methyl-1H-imidazol-1-yl)pyridin-2-amine (62.0 mg, 0.30 mmol) in DME (3 mL) was added to a microwave vial containing palladium(II) acetate (6.82 mg, 0.03 mmol), 2-(Dicyclohexylphosphino)biphenyl (10.64 mg, 0.03 mmol) and CS2CO3 (297 mg, 0.91 mmol) under an athmosphere of argon. The resulting mixture was heated to 100°C in a microwave apparatus for 2 h. The reaction mixture was diluted with dichloromethane and methanol and filtered through a plug of Celite. The solvents were evaporated and the residue was purified by HPLC to give 21 mg of the title product (16 % Yield).

Provenance & Evidence