Benzene, 1-(chloromethyl)-2-fluoro- → HCID 57974358、化合物

HRID 1864251ノート

反応式

HRID 1864251 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].[F:29][C:30]1[CH:37]=[CH:36][CH:35]=[CH:34][C:31]=1[CH2:32]Cl>>[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][CH2:32][C:31]1[CH:34]=[CH:35][CH:36]=[CH:37][C:30]=1[F:29]

参加物

3

反応物 2

HCID 9580Benzene, 1-(chloromethyl)-2-fluoro-HCID 69059499HCID 69059499、化合物

生成物 1

HCID 57974358HCID 57974358、化合物収率 72%

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 2-fluorobenzyl chloride to give the title compound in 72% yield; NMR spectrum (DMSO-d6) 1.37 (d, 3H), 1.94 (s, 3H), 3.04 (s, 3H), 3.30 (1H obscured by H2O), 4.20 (dd, 1H), 5.07 (m, 1H), 5.25 (s, 2H), 7.27 (m, 5H), 7.43 (m, 1H), 7.59 (t, 1H), 7.67 (dd, 1H), 7.70 (t, 1H), 8.07 (d, 1H), 8.45 (s, 1H), 9.93 (s, 1H); Mass Spectrum MH+ 509.

出典と根拠

ORDレコード
ord-16a566cbfb534db3800a7386a6d85aef
出典データセット
uspto-grants-2009_12
特許番号
US07625908B2

反応ノート

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