Reacción #407

Ecuación de reacción

Cc1csc(C2CN(C)Cc3ccc

COc1nc(N)ccc1-c1cnn(

→

COc1nc(Nc2ccc3c(n2)O

Rendimiento 56.4%

Disolventes

COCCOC

Condiciones de reacción

Procedimiento

To 8-chloro-4-methyl-2-(4-methylthiazol-2-yl)-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepine (207 mg, 0.70 mmol) in DME (3 mL) were 6-methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-amine (143 mg, 0.70 mmol), cesium carbonate (342 mg, 1.05 mmol), 2-(Dicyclohexylphosphino)biphenyl (24.53 mg, 0.07 mmol) and Palladium acetate (15.71 mg, 0.07 mmol) added. The reaction was heated to 110°C for 60 min under N2 atmosphere. The solids were filtered off and washed with DCM, the solvents were evaporated and the crude product was purified by silica flash chromatography using DCM : [DCM:MeOH:NH3 = 90:10:1] = 100:0 to 35:65 as gradient. The title compound was obtained as yellow foam.

Fuente