反応 #162099

反応方程式

5-Chloro-3-(5-fluoro-4-methylsulfinyl-pyrimidin-2-yl)-1-(p-tolylsulfonyl)pyrrolo[2,3-b]pyridine

(1S,2S)-cyclohexane-1,2-diamine

→

15b

(1S,2S)—N1-(2-(5-chloro-1-tosyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-yl)cyclohexane-1,2-diamine

溶媒

THF

反応条件

後処理

1. 1
   その他The solvent was evaporated in vacuo
2. 2
   その他the residue was purified by silica gel chromatography (0%-15% MeOH/CH2Cl2)

実験手順

5-Chloro-3-(5-fluoro-4-methylsulfinyl-pyrimidin-2-yl)-1-(p-tolylsulfonyl)pyrrolo[2,3-b]pyridine, 15a, (0.25 g, 0.53 mmol) and (1S,2S)-cyclohexane-1,2-diamine (0.12 g, 1.08 mmol) were dissolved in THF (3.0 mL), and heated to 140° C. for 20 minutes in a sealed vial. The solvent was evaporated in vacuo and the residue was purified by silica gel chromatography (0%-15% MeOH/CH2Cl2) to provide product, 15b, as a white foamy solid (220 mg, 79% yield).

出典