HCID 68682368、化合物 → N-{3-[3-(2-Chloro-4-pyrimidinyl)-6-methylpyrazolo[1,5-a]pyridin-2-yl]phenyl}-2,2,2-trifluoroacetamide

HRID 1157647

反応式

HRID 1157647 の反応式
[Cl:1][C:2]1[N:7]=[C:6]([CH:8]=[CH:9][C:10]2[CH:11]=[C:12]([NH:16][C:17](=[O:22])[C:18]([F:21])([F:20])[F:19])[CH:13]=[CH:14][CH:15]=2)[CH:5]=[CH:4][N:3]=1.[N+]([O-])([O-])=O.[NH2:27][N+:28]1[CH:33]=[CH:32][CH:31]=[C:30]([CH3:34])[CH:29]=1>>[Cl:1][C:2]1[N:7]=[C:6]([C:8]2[C:9]([C:10]3[CH:11]=[C:12]([NH:16][C:17](=[O:22])[C:18]([F:19])([F:20])[F:21])[CH:13]=[CH:14][CH:15]=3)=[N:27][N:28]3[CH:29]=[C:30]([CH3:34])[CH:31]=[CH:32][C:33]=23)[CH:5]=[CH:4][N:3]=1

参加物

3

反応物 2

HCID 68682368HCID 68682368、化合物HCID 86631082HCID 86631082、化合物

生成物 1

HCID 57737199N-{3-[3-(2-Chloro-4-pyrimidinyl)-6-methylpyrazolo[1,5-a]pyridin-2-yl]phenyl}-2,2,2-trifluoroacetamide収率 21.3%

実験手順

N-[3-(2-Chloro-pyrimidin-4-ylethenyl)-phenyl]-2,2,2-trifluoro-acetamide (5.00 g, 18.45 mmol) and 1-amino-3-methylpyridinium nitrate (6.19 g, 36.90 mmol) were combined in a procedure analogous to Example 67, Step A to afford 1.80 g of crude material, which was purified via HPLC separation to give N-{3-[3-(2-chloro-4-pyrimidinyl)-6-methylpyrazolo[1,5-a]pyridin-2-yl]phenyl}-2,2,2-trifluoroacetamide (1.70 g, 21%). 1H NMR (400 MHz, DMSO-d6) δ 11.37 (s, 1H), 8.73 (s, 1H), 8.43 (d, J=5.6 Hz, 1H), 8.28 (d, J=9.2 Hz, 1H), 7.92 (s, 1H), 7.83 (d, J=8.4 Hz, 1H), 7.56-7.49 (m, 2H), 7.45-7.40 (m, 1H), 7.03 (d, J=5.6 Hz, 1H), 2.37 (s, 3H).

後処理

  1. customto afford 1.80 g of crude material, which
  2. customwas purified via HPLC separation

出典と根拠

ORDレコード
ord-06e9dad7154a484181670fb92e408806
出典データセット
uspto-grants-2010_10
特許番号
US07807673B2

関連ノート

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