Sodium ethoxide → HCID 57787998、化合物
反応式
[CH2:1]([O:3][C:4]([C:6]1[CH:7]=[C:8]2[C:13](=[CH:14][C:15]=1[O:16][CH2:17][C:18]1[CH:23]=[CH:22][CH:21]=[C:20]([S:24]([CH3:32])(=[N:26]C(OCC)=O)=[O:25])[CH:19]=1)[N:12]=[CH:11][N:10]=[C:9]2[NH:33][C:34]1[S:35][CH:36]=[CH:37][N:38]=1)=[O:5])[CH3:2].[O-]CC.[Na+]>>[CH3:32][S:24]([C:20]1[CH:19]=[C:18]([CH:23]=[CH:22][CH:21]=1)[CH2:17][O:16][C:15]1[CH:14]=[C:13]2[C:8]([C:9]([NH:33][C:34]3[S:35][CH:36]=[CH:37][N:38]=3)=[N:10][CH:11]=[N:12]2)=[CH:7][C:6]=1[C:4]([O:3][CH2:1][CH3:2])=[O:5])(=[NH:26])=[O:25]参加物
3
実験手順
According to GWP 6, ethyl-7-({(RS)-3-[N-(ethoxycarbonyl)-S-methyl-sulphonimidoyl]-benzyl}oxy)-4-(thiazol-2-ylamino)quinazoline-6-carboxylate (175 mg, 0.182 mmol) is reacted at 80° C. for 2 hours with sodium ethoxide (55 mg, 0.8 mmol). After cooling, the reaction mixture is concentrated to dryness. The residue is taken up in ethyl acetate and water. The organic phase is separated off, dried over sodium sulphate and subsequently concentrated. The desired product is obtained after chromatographic purification (silica gel, dichloromethane/methanol: 9/1) in 42% yield (39 mg).
後処理
- temperatureAfter cooling
- concentrationthe reaction mixture is concentrated to dryness
- customThe organic phase is separated off