Trifluoroacetic acid → 5-Amino-4-[3-(carboxymethyloxy)benzoyl]-1-(4-fluorophenyl)pyrazole

HRID 1278874노트

반응식

HRID 1278874 반응식
[NH2:1][C:2]1[N:6]([C:7]2[CH:12]=[CH:11][C:10]([F:13])=[CH:9][CH:8]=2)[N:5]=[CH:4][C:3]=1[C:14](=[O:30])[C:15]1[CH:20]=[CH:19][CH:18]=[C:17]([O:21][CH2:22][C:23]([O:25]C(C)(C)C)=[O:24])[CH:16]=1.FC(F)(F)C(O)=O>C(Cl)Cl>[NH2:1][C:2]1[N:6]([C:7]2[CH:8]=[CH:9][C:10]([F:13])=[CH:11][CH:12]=2)[N:5]=[CH:4][C:3]=1[C:14](=[O:30])[C:15]1[CH:20]=[CH:19][CH:18]=[C:17]([O:21][CH2:22][C:23]([OH:25])=[O:24])[CH:16]=1

참가 물질

4

반응물 2

HCID 6422Trifluoroacetic acidHCID 98228865-Amino-4-[3-(tert-butoxycarbonylmethyloxy)benzoyl]-1-(4-fluorophenyl)pyrazole

생성물 1

HCID 98849735-Amino-4-[3-(carboxymethyloxy)benzoyl]-1-(4-fluorophenyl)pyrazole수율 68.2%

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

A mixture of 5-amino-4-[3-(tert-butoxycarbonylmethyloxy)benzoyl]-1-(4-fluorophenyl)pyrazole (1.0 g, 3.3 mmol) and trifluoroacetic acid (15 mnl, 194 mmol ) in methylene chloride (15 ml) was stirred overnight at room temperature. The organics were removed in vacuo and the residue was dissolved in toluene. The solution was concentrated and the residue was triturated between ethyl acetate and hexane to give 5-amino-4-[3-(carboxymethyloxy)benzoyl]-1-(4-fluorophenyl)pyrazole (0.8 g) as a solid.

후처리

  1. customThe organics were removed in vacuo
  2. dissolutionthe residue was dissolved in toluene
  3. concentrationThe solution was concentrated
  4. customthe residue was triturated between ethyl acetate and hexane

출처 및 근거

ORD 기록
ord-a526ddf9cd1445709274bc064892850a
출처 데이터셋
uspto-grants-2002_09
특허 번호
US06444696B1

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