5-fluoro-1H-indazol-3-amine → [2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(5-fluoro-1H-indazol-3-yl)-amine

反応式

Cl[C:2]1[C:3]2[CH:18]=[CH:17][CH:16]=[N:15][C:4]=2[N:5]=[C:6]([C:8]2[CH:13]=[CH:12][CH:11]=[CH:10][C:9]=2[Cl:14])[N:7]=1.[F:19][C:20]1[CH:21]=[C:22]2[C:26](=[CH:27][CH:28]=1)[NH:25][N:24]=[C:23]2[NH2:29]>>[Cl:14][C:9]1[CH:10]=[CH:11][CH:12]=[CH:13][C:8]=1[C:6]1[N:7]=[C:2]([NH:29][C:23]2[C:22]3[C:26](=[CH:27][CH:28]=[C:20]([F:19])[CH:21]=3)[NH:25][N:24]=2)[C:3]2[CH:18]=[CH:17][CH:16]=[N:15][C:4]=2[N:5]=1

参加物

反応物 2

HCID 43278965-fluoro-1H-indazol-3-amine

HCID 219392444-Chloro-2-(2-chloro-phenyl)-pyrido(2,3-d]pyrimidine

生成物 1

HCID 21939157[2-(2-Chloro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(5-fluoro-1H-indazol-3-yl)-amine

実験手順

Prepared from 4-Chloro-2-(2-chloro-phenyl)-pyrido[2,3-d]pyrimidine (100 mg, 0.36 mmol) and 5-Fluoro-1H-indazol-3-ylamine (108 mg, 0.72 mmol). Purification by preparative HPLC afforded the title compound as a yellow, di-TFA salt (45 mg, 22% yield). HPLC-Method A, Rt 3.00 min; 1H NMR (DMSO, 500 MHz): δ13.0 (1H, s), 10.90(1H, bs), 9.15-9.05 (2H, m), 7.70 (1H, m), 7.60-7.30 (6H, m), 7.20 (1H, m); MS (m/z), MH+ 391.1.

後処理

customPurification by preparative HPLC

出典と根拠

ORDレコード: ord-a8aa1666376641e0abfdecf0bbe0375a
出典データセット: uspto-grants-2003_08
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US06610677B2

反応ノート

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