반응 #62327

반응 방정식

water

3-[(E)-2-(4-fluorophenyl)-vinyl]-4-[2-(tetrahydropyran-2-yloxy)-ethoxy]-1H-indazole-1,5-dicarboxylic acid 1-tert-butyl ester 5-ethyl ester

hydrochloric acid

→

title compound

수율 69.8%

3-[(E)-2-(4-Fluorophenyl)-vinyl]-4-(2-hydroxyethoxy)-1H-indazole-1,5-dicarboxylic acid 1-tert-butyl ester 5-ethyl ester

수율 69.8%

용매

tetrahydrofuran

반응 조건

후처리

1. 1
   추출extracted twice ethyl acetate
2. 2
   세척the resultant organic layer was washed once with saturated brine
3. 3
   건조dried over magnesium sulfate
4. 4
   기타The solvent was evaporated
5. 5
   기타the crude product was purified
6. 6
   기타separated by silica gel column chromatography

실험 절차

To a solution of 147 mg of 3-[(E)-2-(4-fluorophenyl)-vinyl]-4-[2-(tetrahydropyran-2-yloxy)-ethoxy]-1H-indazole-1,5-dicarboxylic acid 1-tert-butyl ester 5-ethyl ester in 1.5 mL of tetrahydrofuran was added 1.5 mL of 2N hydrochloric acid, and stirred at room temperature for 19 hours. Thereafter, the reaction solution was added with water and extracted twice ethyl acetate, and the resultant organic layer was washed once with saturated brine, and dried over magnesium sulfate. The solvent was evaporated, and the crude product was purified and separated by silica gel column chromatography, to afford 87.1 mg of the title compound as a colorless oil.

출처