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

HRID 512863노트

반응식

HRID 512863 반응식
[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

참가 물질

4

반응물 2

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

생성물 1

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

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

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.

후처리

  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

출처 및 근거

ORD 기록
ord-05a761273e034f1fb71ef13db4eae075
출처 데이터셋
uspto-grants-2015_08
특허 번호
US09102669B2

반응 노트

불러오는 중…