1-[(2-methyl-1,3-thiazol-5-yl)methyl]-1H-indazol-5-amine → (2R)-N,N-dimethyl-2-{[4-({1-[(2-methyl-1,3-thiazol-5-yl)methyl]-1H-indazol-5-yl}amino)quinazolin-5-yl]oxy}propanamide

HRID 1162231노트

반응식

HRID 1162231 반응식
[CH3:1][N:2]([CH3:19])[C:3](=[O:18])[C@H:4]([O:6][C:7]1[CH:16]=[CH:15][CH:14]=[C:13]2[C:8]=1[C:9](=O)[NH:10][CH:11]=[N:12]2)[CH3:5].[CH3:20][C:21]1[S:22][C:23]([CH2:26][N:27]2[C:35]3[C:30](=[CH:31][C:32]([NH2:36])=[CH:33][CH:34]=3)[CH:29]=[N:28]2)=[CH:24][N:25]=1>>[CH3:1][N:2]([CH3:19])[C:3](=[O:18])[C@H:4]([O:6][C:7]1[CH:16]=[CH:15][CH:14]=[C:13]2[C:8]=1[C:9]([NH:36][C:32]1[CH:31]=[C:30]3[C:35](=[CH:34][CH:33]=1)[N:27]([CH2:26][C:23]1[S:22][C:21]([CH3:20])=[N:25][CH:24]=1)[N:28]=[CH:29]3)=[N:10][CH:11]=[N:12]2)[CH3:5]

참가 물질

3

반응물 2

HCID 686192981-[(2-methyl-1,3-thiazol-5-yl)methyl]-1H-indazol-5-amineHCID 136346624(2R)-N,N-dimethyl-2-[(4-oxo-3,4-dihydroquinazolin-5-yl)oxy]propanamide

생성물 1

HCID 16117350(2R)-N,N-dimethyl-2-{[4-({1-[(2-methyl-1,3-thiazol-5-yl)methyl]-1H-indazol-5-yl}amino)quinazolin-5-yl]oxy}propanamide수율 61.5%

실험 절차

Using the same procedure as in Example 18, (2R)—N,N-dimethyl-2-[(4-oxo-3,4-dihydroquinazolin-5-yl)oxy]propanamide (261 mg, 1 mmol) and 1-[(2-methyl-1,3-thiazol-5-yl)methyl]-1H-indazol-5-amine (269 mg, 1.1 mmol) were reacted to give the title compound as a white solid (300 mg, 61%); NMR Spectrum (CDCl3) 1.73 (d, 3H), 2.62 (s, 3H), 3.07 (s, 3H), 3.15 (s, 3H), 5.43 (q, 1H), 5.71 (s, 2H), 6.82 (d, 1H), 7.43 (d, 1H), 7.49 (d, 1H), 7.61 (m, 2H), 7.86 (dd, 1H), 8.05 (s, 1H), 8.42 (s, 1H), 8.62 (s, 1H); Mass spectrum 488.

후처리

  1. customwere reacted

출처 및 근거

ORD 기록
ord-07fbc0180d9747c3865aef043536f1ab
출처 데이터셋
uspto-grants-2010_10
특허 번호
US07820683B2

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