1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-amine → (R)-N,N-dimethyl-2-(4-(1-(thiazol-2-ylmethyl)-1H-indazol-5-ylamino)quinazolin-5-yloxy)propanamide

HRID 1162230ノート

反応式

HRID 1162230 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].[S:20]1[CH:24]=[CH:23][N:22]=[C:21]1[CH2:25][N:26]1[C:34]2[C:29](=[CH:30][C:31]([NH2:35])=[CH:32][CH:33]=2)[CH:28]=[N:27]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:35][C:31]1[CH:30]=[C:29]3[C:34](=[CH:33][CH:32]=1)[N:26]([CH2:25][C:21]1[S:20][CH:24]=[CH:23][N:22]=1)[N:27]=[CH:28]3)=[N:10][CH:11]=[N:12]2)[CH3:5]

参加物

3

反応物 2

HCID 686192881-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-amineHCID 136346624(2R)-N,N-dimethyl-2-[(4-oxo-3,4-dihydroquinazolin-5-yl)oxy]propanamide

生成物 1

HCID 16117349(R)-N,N-dimethyl-2-(4-(1-(thiazol-2-ylmethyl)-1H-indazol-5-ylamino)quinazolin-5-yloxy)propanamide収率 77.1%

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 (150 mg, 0.57 mmol) and 1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-amine (138 mg, 0.6 mmol) were reacted to give the title compound as a white solid (208 mg, 77%); NMR Spectrum (CDCl3) 1.73 (d, 3H), 3.06 (s, 3H), 3.14 (s, 3H), 5.43 (q, 1H), 5.92 (s, 2H), 6.82 (d, 1H), 7.26 (m, 1H), 7.50 (d, 2H), 7.61 (t, 1H), 7.75 (d, 1H), 7.87 (dd, 1H), 8.11 (s, 1H), 8.45 (s, 1H), 8.62 (s, 1H); Mass spectrum 474.

後処理

  1. customwere reacted

出典と根拠

ORDレコード
ord-67c836bd132b4dcf894a49bea5b1eb64
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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