Hydrochloric Acid → 4-(7-Benzofuranylamino)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazoline
반응식
Cl[C:2]1[C:11]2[C:6](=[CH:7][C:8]([O:14][CH2:15][CH2:16][CH2:17][N:18]3[CH2:23][CH2:22][N:21]([CH3:24])[CH2:20][CH2:19]3)=[C:9]([O:12][CH3:13])[CH:10]=2)[N:5]=[CH:4][N:3]=1.[NH2:25][C:26]1[C:34]2[O:33][CH:32]=[CH:31][C:30]=2[CH:29]=[CH:28][CH:27]=1.Cl>C(O)(C)C>[O:33]1[C:34]2[C:26]([NH:25][C:2]3[C:11]4[C:6](=[CH:7][C:8]([O:14][CH2:15][CH2:16][CH2:17][N:18]5[CH2:23][CH2:22][N:21]([CH3:24])[CH2:20][CH2:19]5)=[C:9]([O:12][CH3:13])[CH:10]=4)[N:5]=[CH:4][N:3]=3)=[CH:27][CH:28]=[CH:29][C:30]=2[CH:31]=[CH:32]1참가 물질
반응 조건
- 온도
- 85 °C
실험 절차
A mixture of 4-chloro-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazoline (0.1 g), 7-aminobenzofuran (0.057 g), isopropanol (4 ml) and a solution of hydrogen chloride in isopropanol (6M, 0.06 ml) was stirred and heated to 85° C. for 3 hours. The resultant mixture was cooled to ambient temperature and the precipitate was isolated by filtration, washed in turn with a 1:1 mixture of diethyl ether and isopropanol and with diethyl ether and dried under vacuum. There was thus obtained the title compound (0.09 g) as a dihydrochloride salt; NMR Spectrum: (DMSOd6 and CF3COOD) 2.35 (m, 2H), 2.9 (s, 3H), 3.45 (br m, 5H), 3.8 (br m, 5H), 4.05 (s, 3H), 4.35 (t, 2H), 7.1 (d, 1H), 7.45 (m, 3H), 7.75 (d, 1H), 8.05 (s, 1H), 8.25 (s, 1H), 8.8 (s, 1H); Mass Spectrum: M+H+ 448.
후처리
- customthe precipitate was isolated by filtration
- washwashed in turn with a 1:1 mixture of diethyl ether and isopropanol and with diethyl ether
- customdried under vacuum
출처 및 근거
- ORD 기록
- ord-9afff1b7f8194970a2c866143330cf5a
- 출처 데이터셋
- uspto-grants-2005_02
- 특허 번호
- US06849625B2
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