Dimethylformamide → HCID 178505514、化合物

HRID 1023207

反応式

HRID 1023207 の反応式
[F:1][C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][C:3]=1[C:8]1[NH:16][C:11]2=[CH:12][N:13]=[CH:14][CH:15]=[C:10]2[CH:9]=1.[OH-:17].[Na+].Cl[CH2:20][C:21]1[O:25][N:24]=[C:23]([C:26]2[CH:31]=[CH:30][C:29]([F:32])=[CH:28][C:27]=2[C:33]([F:36])([F:35])[F:34])[CH:22]=1.CN([CH:40]=[O:41])C>>[F:34][C:33]([F:36])([F:35])[C:40]([O-:41])=[O:17].[F:1][C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][C:3]=1[C:8]1[CH:9]=[C:10]2[CH:15]=[CH:14][N:13]([CH2:20][C:21]3[O:25][N:24]=[C:23]([C:26]4[CH:31]=[CH:30][C:29]([F:32])=[CH:28][C:27]=4[C:33]([F:36])([F:34])[F:35])[CH:22]=3)[CH:12]=[C:11]2[NH+:16]=1

参加物

5

反応物 4

HCID 6228Dimethylformamide2 回HCID 14798Sodium HydroxideHCID 468639965-Chloromethyl-3-(4-fluoro-2-trifluoromethyl-phenyl)-isoxazoleHCID 574382742-(2-Fluoro-phenyl)-1H-pyrrolo[2,3-c]pyridine

生成物 1

HCID 178505514HCID 178505514、化合物収率 81%

実験手順

To a solution of 2-(2-Fluoro-phenyl)-1H-pyrrolo[2,3-c]pyridine (50 mg, 0.244 mmole) in DMF (1 ml) was added 10% (w/v) aqueous NaOH (113 μl, 0.28 mmole) followed by a solution of 5-Chloromethyl-3-(4-fluoro-2-trifluoromethyl-phenyl)-isoxazole (79 mg, 0.28 mmole) in DMF (0.5 ml). The reaction mixture was stirred at room temperature for 12 hours. The crude reaction mixture was purified by reverse phase HPLC with mass directed collection. Obtained 109 mg (81%) of 2-(2-Fluoro-phenyl)-6-[3-(4-fluoro-2-trifluoromethyl-phenyl)-isoxazol-5-ylmethyl]-6H-pyrrolo[2,3-c]pyridinium trifluoroacetate.

後処理

  1. customThe crude reaction mixture
  2. customwas purified by reverse phase HPLC with mass
  3. customcollection

出典と根拠

ORDレコード
ord-a21b4833ad694661919841c2c88c0b67
出典データセット
uspto-grants-2014_05
特許番号
US08722677B2

関連ノート

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