反応 #419903

反応方程式

(R)-2-(6-chloro-5-cyanopyrazin-2-ylamino)-4-methylpentanamide

4-amino-N-methyl-indole

K2CO3

BINAP

→

(R)-2-(5-cyano-6-(1-methyl-1H-indol-4-ylamino)pyrazin-2-ylamino)-4-methylpentanamide

溶媒

dioxane

反応条件

後処理

1. 1
   その他was degassed with Ar
2. 2
   workup.ADDITIONWater and EtOAc were added
3. 3
   その他Organic phase was separated
4. 4
   乾燥dried over Na2SO4
5. 5
   濃縮concentrated in vacuo

実験手順

A mixture of (R)-2-(6-chloro-5-cyanopyrazin-2-ylamino)-4-methylpentanamide (80 mg, 0.299 mmol), 4-amino-N-methyl-indole (62 mg, 0.424 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, dried over Na2SO4, concentrated in vacuo to give (R)-2-(5-cyano-6-(1-methyl-1H-indol-4-ylamino)pyrazin-2-ylamino)-4-methylpentanamide as a crude residue (151 mg).

出典