反应 #163078

反应方程式

(S)-6-chloro-N-(1-(4-fluorophenyl)ethyl)-3-nitropyridin-2-amine

5-isopropoxy-1H-pyrazol-3-amine

DIEA

→

title compound

收率 22.0%

(S)—N2-(1-(4-Fluorophenyl)ethyl)-N6-(5-isopropoxy-1H-pyrazol-3-yl)-3-nitropyridine-2,6-diamine

收率 22.0%

溶剂

n-BuOH

反应条件

后处理

1. 1
   其他The solvent was removed under reduced pressure
2. 2
   其他the residue was purified by chromatography (hexane-EtOAc=3:1)

实验过程

A mixture of (S)-6-chloro-N-(1-(4-fluorophenyl)ethyl)-3-nitropyridin-2-amine (Method 30, 1.08 g, 3.7 mmol), 5-isopropoxy-1H-pyrazol-3-amine (0.57 g, 4.0 mmol), and DIEA (0.80 ml, 4.6 mmol) in n-BuOH (10 ml) was heated in a sealed tube at 115° C. for 72 hours. The solvent was removed under reduced pressure and the residue was purified by chromatography (hexane-EtOAc=3:1) to give the title compound as a yellow solid (0.32 g, 22%). MS: Calcd.: 400. Found: [M+H]+ 401.

来源