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 1162231ノート

反応式

HRID 1162231 の反応式
[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]

参加物

3

反応物 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

生成物 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}propanamide収率 61.5%

実験手順

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.

後処理

  1. customwere reacted

出典と根拠

ORDレコード
ord-07fbc0180d9747c3865aef043536f1ab
出典データセット
uspto-grants-2010_10
特許番号
US07820683B2

反応ノート

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