反应 #9312

反应方程式

p-Toluenesulfonic acid hydrate

epifluorohydrin

N-cyclopropylmethyl-N-[7-(2-methoxy-4,6-dimethylphenyl)-2-(methylsulfanyl)pyrazolo[1,5-a]pyridin-3-yl]amine

→

title compound

1-(Cyclopropylmethyl)[7-(2-methoxy-4,6-dimethylphenyl)-2-(methylsulfanyl)pyrazolo[1,5-a]pyridin-3-yl]amino-3-fluoro-2-propanol

溶剂

1,2-dimethoxyethane

反应条件

后处理

1. 1
   温度the mixture was heated
2. 2
   温度to reflux for 3 hours
3. 3
   workup.DISTILLATIONthe solvent was distilled off under reduced pressure
4. 4
   其他The obtained residue was purified by basic silica gel column chromatography (ethyl acetate:n-hexane=1:5)

实验过程

p-Toluenesulfonic acid hydrate (40 mg) and epifluorohydrin (0.15 mL) [CAS No.503-09-3] were added to a solution of N-cyclopropylmethyl-N-[7-(2-methoxy-4,6-dimethylphenyl)-2-(methylsulfanyl)pyrazolo[1,5-a]pyridin-3-yl]amine (50 mg) in 1,2-dimethoxyethane (0.40 mL), and the mixture was heated to reflux for 3 hours. After cooling to room temperature, the solvent was distilled off under reduced pressure. The obtained residue was purified by basic silica gel column chromatography (ethyl acetate:n-hexane=1:5) to obtain the title compound (24 mg) as a brownish oil.

来源