반응 #407

ord-980427b3cc854bc88aa11ec4ee256fb1

반응 방정식

Cc1csc(C2CN(C)Cc3ccc(Cl)nc3O2)n1
Cc1csc(C2CN(C)Cc3ccc
COc1nc(N)ccc1-c1cnn(C)c1
COc1nc(N)ccc1-c1cnn(
COc1nc(Nc2ccc3c(n2)OC(c2nc(C)cs2)CN(C)C3)ccc1-c1cnn(C)c1
COc1nc(Nc2ccc3c(n2)O
수율 56.4%

용매

반응 조건

온도
110°CELSIUS

실험 절차

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.

출처

750 AstraZeneca ELN dataset