반응 #166199

반응 방정식

4-(2-fluoro-4-iodophenylamino)-1-(toluene-4-sulfonyl)-1H-indazole-5-carboxylic acid methyl ester

bis(tributyltin) oxide

→

title compound

수율 92.0%

4-(2-Fluoro-4-iodo-phenylamino)-1-(toluene-4-sulfonyl)-1H-indazole-5-carboxylic acid

수율 92.0%

용매

toluene

반응 조건

후처리

1. 1
   온도the reaction mixture heated
2. 2
   온도at reflux for 48 hours
3. 3
   농축The reaction mixture was concentrated in vacuo

실험 절차

To a solution of 4-(2-fluoro-4-iodophenylamino)-1-(toluene-4-sulfonyl)-1H-indazole-5-carboxylic acid methyl ester (0.51 g, 0.91 mmol) in toluene (5 mL) was added bis(tributyltin) oxide (0.92 mL, 1.8 mmol) and the reaction mixture heated at reflux for 48 hours. The reaction mixture was concentrated in vacuo and the resultant residue subjected to flash chromatography (Si—PPC, gradient 0-10% methanol in DCM) to yield the title compound as a light brown solid (0.46 g, 92%). LCMS (Method B): RT=4.27 min, [M+H]+=552.

출처