反应详情

To crude ethyl 1-(3-chlorobenzyl)-3-(4-chlorophenyl)-5-(trifluoromethyl)-1H-pyrrole-2-carboxylate (732 mg, max. 1.57 mmol) in EtOH (2 mL) and H2O (2 mL) was added LiOH.H2O (347 mg, 8.28 mmol). The reaction mixture was stirred at reflux temperature overnight. The reaction mixture was concentrated, diluted with H2O (5 mL) and acidified with aqueous 1 M KHSO4 (10 mL) while cooling with an ice-bath. The precipitate was filtrated, washed with H2O (2×) and dried on filter to give ACI-07 (533 mg, 82% over two steps).

1. temperatureat reflux temperature overnight
2. concentrationThe reaction mixture was concentrated
3. additiondiluted with H2O (5 mL)
4. temperaturewhile cooling with an ice-bath
5. filtrationThe precipitate was filtrated
6. washwashed with H2O (2×)
7. customdried
8. filtrationon filter
9. customto give ACI-07 (533 mg, 82% over two steps)