反応 #504

ord-2b09b0edd9af4f8e80b89621d51beb35

反応方程式

CN1Cc2ccc(Cl)nc2O[C@H](c2ccccc2)C1
CN1Cc2ccc(Cl)nc2O[C@
COc1nc(N)ccc1-c1ccc(=O)n(C)c1
COc1nc(N)ccc1-c1ccc(
COc1nc(Nc2ccc3c(n2)O[C@H](c2ccccc2)CN(C)C3)ccc1-c1ccc(=O)n(C)c1
COc1nc(Nc2ccc3c(n2)O
収率 35.1%

溶媒

反応条件

温度
120°CELSIUS

実験手順

(R)-8-chloro-4-methyl-2-phenyl-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepine (300 mg, 1.09 mmol), 5-(6-amino-2-methoxypyridin-3-yl)-1-methylpyridin-2(1H)-one (253 mg, 1.09 mmol), Palladium(II) acetate (24.51 mg, 0.11 mmol), 9,9-Dimethyl-4,5-bis(diphenylphosphino)xanthene (63.2 mg, 0.11 mmol) and Sodium tert-pentoxide (144 mg, 1.31 mmol) were mixed in dioxane (3 mL) and run in a microwave reactor for 40 min at 120°C. the mixture was filtered thru celite and concetrated. purified using flash column chromatography using 0-6 % MeOH (1% NH3) in DCM.

出典

750 AstraZeneca ELN dataset