反应详情

A mixture of tert-butyl (1S,2R)-2-(6-chloro-5-cyanopyrazin-2-ylamino)cyclohexylcarbamate (80 mg, 0.227 mmol), 1-methyl-1H-indol-4-amine (50 mg, 0.342 mmol), K2CO3 (65 mg, 0.471 mmol), BINAP (25 mg, 0.040 mmol) and Pd(OAc)2 (10 mg, 0.044 mmol) in dioxane (2 mL) was degassed with Ar, then was stirred at 100 C for 20 h. Water and EtOAc were added. Organic phase was separated. The aqueous phase was extracted with EtOAc again. The combined organic phases were dried over Na2SO4, concentrated in vacuo to give a crude tert-butyl (1S,2R)-2-(5-cyano-6-(1-methyl-1H-indol-4-ylamino)pyrazin-2-ylamino)cyclohexylcarbamate (153 mg).

1. customwas degassed with Ar
2. additionWater and EtOAc were added
3. customOrganic phase was separated
4. extractionThe aqueous phase was extracted with EtOAc again
5. dry with materialThe combined organic phases were dried over Na2SO4
6. concentrationconcentrated in vacuo