Trifluoroacetic acid → 6-fluoro-1-(piperidin-4-yl)-1H-indazole

HRID 512863ノート

反応式

HRID 512863 の反応式
[F:1][C:2]1[CH:10]=[C:9]2[C:5]([CH:6]=[N:7][N:8]2[CH:11]2[CH2:16][CH2:15][N:14](C(OC(C)(C)C)=O)[CH2:13][CH2:12]2)=[CH:4][CH:3]=1.C(O)(C(F)(F)F)=O>C(Cl)Cl>[F:1][C:2]1[CH:10]=[C:9]2[C:5]([CH:6]=[N:7][N:8]2[CH:11]2[CH2:16][CH2:15][NH:14][CH2:13][CH2:12]2)=[CH:4][CH:3]=1

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 89614504tert-butyl 4-(6-fluoro-1H-indazol-1-yl)piperidine-1-carboxylate

生成物 1

HCID 539239646-fluoro-1-(piperidin-4-yl)-1H-indazole

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

To tert-butyl 4-(6-fluoro-1H-indazol-1-yl)piperidine-1-carboxylate prepared as in STEP 1 above (998 mg, 3.10 mmol) in DCM (20 mL) at 0° C. was added TFA (10 mL). The resulting mixture was then stirred for 1 hour. The solvent was removed in vacuo. To the resulting residue was added 0.5N NaOH (15 mL), followed repeated extraction with CHCl3. The organic layer was dried with MgSO4 and filtered to yield 6-fluoro-1-(piperidin-4-yl)-1H-indazole.

後処理

  1. customThe solvent was removed in vacuo
  2. additionTo the resulting residue was added 0.5N NaOH (15 mL)
  3. extractionextraction with CHCl3
  4. dry with materialThe organic layer was dried with MgSO4
  5. filtrationfiltered

出典と根拠

ORDレコード
ord-05a761273e034f1fb71ef13db4eae075
出典データセット
uspto-grants-2015_08
特許番号
US09102669B2

反応ノート

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