Acetic Acid → 9-Bromo-5-methyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetic acid
反応式
[Br:1][C:2]1[C:3]2[C:4]3[C:15](CC#N)=[N:14][N:13]([C:19]4[CH:24]=[CH:23][CH:22]=[CH:21][CH:20]=4)[C:12](=[O:25])[C:5]=3[N:6]([CH3:11])[C:7]=2[CH:8]=[CH:9][CH:10]=1.Cl.[C:27]([OH:30])(=[O:29])[CH3:28]>>[Br:1][C:2]1[C:3]2[C:4]3[C:15]([CH2:28][C:27]([OH:30])=[O:29])=[N:14][N:13]([C:19]4[CH:20]=[CH:21][CH:22]=[CH:23][CH:24]=4)[C:12](=[O:25])[C:5]=3[N:6]([CH3:11])[C:7]=2[CH:8]=[CH:9][CH:10]=1参加物
実験手順
A solution of 4.8 g (12.2 mmol) of 9-bromo-5-methyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetonitrile in a mixture of 190 ml of acetic acid and of 50 ml of concentrated hydrochloric acid is heated at reflux for 6 h. The solution is concentrated under reduced pressure and the residue is taken up in a mixture of dichloromethane and of water. Basification is carried out with 30% sodium hydroxide solution, separation is carried out by settling and extraction is carried out with dichloromethane. The aqueous phase is acidified with concentrated hydrochloric acid while cooling with an ice bath. The precipitate is collected by filtration, washed with water and dried under reduced pressure. 3.1 g (7.5 mmol) of solid are obtained.
後処理
- temperatureat reflux for 6 h
- concentrationThe solution is concentrated under reduced pressure
- additionthe residue is taken up in a mixture of dichloromethane and of water
- customBasification is carried out with 30% sodium hydroxide solution, separation
- extractionextraction
- temperaturewhile cooling with an ice bath
- filtrationThe precipitate is collected by filtration
- washwashed with water
- customdried under reduced pressure
出典と根拠
- ORDレコード
- ord-bad266f6fea24d97b70184279ff7acc1
- 出典データセット
- uspto-grants-2001_07
- 特許番号
- US06262045B1
反応ノート
読み込み中…