HCID 17904941, 화합물 → 6-Acetoxy-7-methoxy-4-[2-methyl-5-(2-morpholinopyridine-4-carboxamido)anilino]quinazoline Dihydrochloride

HRID 2084017노트

반응식

HRID 2084017 반응식
[NH2:1][C:2]1[CH:3]=[C:4]([NH:9][C:10]([C:12]2[CH:17]=[CH:16][N:15]=[C:14]([N:18]3[CH2:23][CH2:22][O:21][CH2:20][CH2:19]3)[CH:13]=2)=[O:11])[CH:5]=[CH:6][C:7]=1[CH3:8].[ClH:24].[C:25]([O:28][C:29]1[CH:30]=[C:31]2[C:36](=[CH:37][C:38]=1[O:39][CH3:40])[N:35]=[CH:34][N:33]=[C:32]2[Cl:41])(=[O:27])[CH3:26]>C(O)(C)C>[ClH:41].[ClH:24].[C:25]([O:28][C:29]1[CH:30]=[C:31]2[C:36](=[CH:37][C:38]=1[O:39][CH3:40])[N:35]=[CH:34][N:33]=[C:32]2[NH:1][C:2]1[CH:3]=[C:4]([NH:9][C:10]([C:12]2[CH:17]=[CH:16][N:15]=[C:14]([N:18]3[CH2:19][CH2:20][O:21][CH2:22][CH2:23]3)[CH:13]=2)=[O:11])[CH:5]=[CH:6][C:7]=1[CH3:8])(=[O:27])[CH3:26]

참가 물질

4

반응물 2

HCID 17904941HCID 17904941, 화합물HCID 220221594-Chloro-7-methoxyquinazolin-6-yl acetate--hydrogen chloride (1/1)

생성물 1

HCID 227322476-Acetoxy-7-methoxy-4-[2-methyl-5-(2-morpholinopyridine-4-carboxamido)anilino]quinazoline Dihydrochloride수율 80%

시약·촉매·용매 1

HCID 3776Isopropanol용매

반응 조건

온도
85 °C

실험 절차

A mixture of N-(3-amino-4-methylphenyl)-2-morpholinopyridine-4-carboxamide (178 mg), 6-acetoxy-4-chloro-7-methoxyquinazoline hydrochloride (150 mg) and isopropanol (5 ml) was stirred and heated to 85° C. for 3 hours. The reaction mixture was allowed to cool to ambient temperature and the solid was isolated and washed in turn with isopropanol (5 ml) and isohexane (2×5 ml). There was thus obtained the title compound (249 mg, 80%); NMR: 2.17 (s, 3H), 2.38 (s, 3H), 3.56 (m, 4H), 3.72 (m, 4H), 4.0 (s, 3H), 7.16 (m, 1H), 7.37 (m, 2H), 7.52 (s, 1H), 7.68 (m, 1H), 7.87 (m, 1H), 8.24 (m, 1H), 8.67 (s, 1H), 8.8 (s, 1H), 10.6 (s, 1H), 11.50 (s, 1H); m/s: M+H+ 529.

후처리

  1. temperatureto cool to ambient temperature
  2. customthe solid was isolated
  3. washwashed in turn with isopropanol (5 ml) and isohexane (2×5 ml)

출처 및 근거

ORD 기록
ord-4ebd3b192c98400c8213269fb995b7d1
출처 데이터셋
uspto-grants-2004_04
특허 번호
US06716847B2

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