2,5-Dimethyl-2H-pyrazole-3-carbonyl chloride → N-[3-(3-{2-[(3-Fluorophenyl)amino]-4-pyrimidinyl}pyrazolo[1,5-a]pyridin-2-yl)phenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide

HRID 1159886

反応式

HRID 1159886 の反応式
ClC1C=[CH:38][C:37](F)=[CH:36][C:3]=1[C:4]([NH:6][C:7]1[CH:12]=[CH:11][CH:10]=[C:9]([C:13]2[C:21]([C:22]3[CH:27]=[CH:26][N:25]=[C:24]([NH:28][C:29]4[CH:34]=[CH:33][CH:32]=[C:31]([F:35])[CH:30]=4)[N:23]=3)=[C:16]3[CH:17]=[CH:18][CH:19]=[CH:20][N:15]3[N:14]=2)[CH:8]=1)=[O:5].[CH3:41][N:42]1C(C(Cl)=O)=CC(C)=[N:43]1>>[F:35][C:31]1[CH:30]=[C:29]([NH:28][C:24]2[N:23]=[C:22]([C:21]3[C:13]([C:9]4[CH:8]=[C:7]([NH:6][C:4]([C:3]5[N:42]([CH3:41])[N:43]=[C:37]([CH3:38])[CH:36]=5)=[O:5])[CH:12]=[CH:11][CH:10]=4)=[N:14][N:15]4[CH:20]=[CH:19][CH:18]=[CH:17][C:16]=34)[CH:27]=[CH:26][N:25]=2)[CH:34]=[CH:33][CH:32]=1

参加物

3

反応物 2

HCID 27362992,5-Dimethyl-2H-pyrazole-3-carbonyl chlorideHCID 595137492-Chloro-5-fluoro-N-(3-{3-[2-(3-fluoro-phenylamino)-pyrimidin-4-yl]-pyrazolo[1,5-a]pyridin-2-yl}-phenyl)-benzamide

生成物 1

HCID 59513696N-[3-(3-{2-[(3-Fluorophenyl)amino]-4-pyrimidinyl}pyrazolo[1,5-a]pyridin-2-yl)phenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide

実験手順

In an analogous procedure to Example 11, 40 mg of the title compound was prepared from 79 mg of 1,3-dimethyl-1H-pyrazole-5-carbonyl chloride to give the product as a white solid: 1H NMR (d6-DMSO, 300 MHz) δ 2.23 (s, 3H), 4.02 (s, 3H), 6.62 (d, 1H, J=5.2 Hz), 6.77 (td, 1H, J=9.0 and 2.3 Hz), 6.87 (s, 1H), 7.18 (td, 1H, J=6.9 and 1.3 Hz), 7.29-7.38 (m, 2H), 7.48-7.57 (m, 3H), 7.84 (d, 1H, J=10.8 Hz), 7.93 (d, 1H, J=6.4 Hz), 8.11 (s, 1H), 8.36 (d, 1H, J=5.2 Hz), 8.55 (d, 1H, J=8.8 Hz), 8.90 (d, 1H, J=6.8 Hz), 9.85 (s, 1H), and 10.28 (s, 1H); HRMS calcd for C29H23FN8O: 518.1979, found: 519.2060 (M+H+).

出典と根拠

ORDレコード
ord-a2e0636d18914b83b4e41cd55d447a85
出典データセット
uspto-grants-2010_10
特許番号
US07812022B2

関連ノート

読み込み中…