4-(Chloromethyl)-1,3-thiazole hydrochloride → HCID 57974318、化合物

HRID 1864249ノート

反応式

HRID 1864249 の反応式
[Cl:1][C:2]1[CH:3]=[C:4]([NH:9][C:10]2[C:19]3[C:14](=[CH:15][CH:16]=[CH:17][C:18]=3[O:20][C@H:21]([CH3:28])[CH2:22][N:23]([CH3:27])[C:24](=[O:26])[CH3:25])[N:13]=[CH:12][N:11]=2)[CH:5]=[CH:6][C:7]=1[OH:8].Cl.Cl[CH2:31][C:32]1[N:33]=[CH:34][S:35][CH:36]=1>>[Cl:1][C:2]1[CH:3]=[C:4]([NH:9][C:10]2[C:19]3[C:14](=[CH:15][CH:16]=[CH:17][C:18]=3[O:20][C@H:21]([CH3:28])[CH2:22][N:23]([CH3:27])[C:24](=[O:26])[CH3:25])[N:13]=[CH:12][N:11]=2)[CH:5]=[CH:6][C:7]=1[O:8][CH2:31][C:32]1[N:33]=[CH:34][S:35][CH:36]=1

参加物

3

反応物 2

HCID 27632894-(Chloromethyl)-1,3-thiazole hydrochlorideHCID 69059499HCID 69059499、化合物

生成物 1

HCID 57974318HCID 57974318、化合物収率 17%

実験手順

The procedure described in Example 3 was repeated using N-[(2R)-2-({4-[(3-chloro-4-hydroxyphenyl)amino]quinazolin-5-yl}oxy)propyl]-N-methylacetamide (obtained as described for in Example 50, preparation of starting materials) and 4-(chloromethyl)-thiazole hydrochloride to give the title compound in 17% yield; NMR spectrum (DMSO-d6) 1.36 (d, 3H), 1.94 (s, 3H), 3.02 (s, 3H), 3.3O (1H obscured by H2O), 4.21 (dd, 1H), 5.09 (m, 1H), 5.33 (s, 2H), 7.29 (m, 3H), 7.70 (m, 2H), 7.81 (s, 1H), 8.08 (s, 1H), 8.47 (s, 1H), 9.13 (s, 1H), 9.96 (s, 1H); Mass Spectrum MH+ 498.

出典と根拠

ORDレコード
ord-3a5cdfb4d80a44fa81bde7efb52c4c7d
出典データセット
uspto-grants-2009_12
特許番号
US07625908B2

反応ノート

読み込み中…