1,2-Dichloroethane → 4-(2-Methoxy-benzoylamino)-1H-pyrazole-3-carboxylic acid (4-fluoro-phenyl)-amide

HRID 1624937

반응식

HRID 1624937 반응식
[CH3:1][O:2][C:3]1[CH:11]=[CH:10][CH:9]=[CH:8][C:4]=1[C:5]([OH:7])=O.[F:12][C:13]1[CH:18]=[CH:17][C:16]([NH:19][C:20]([C:22]2[C:26]([NH2:27])=[CH:25][NH:24][N:23]=2)=[O:21])=[CH:15][CH:14]=1.C(Cl)CCl.C1C=CC2N(O)N=NC=2C=1>CN(C=O)C>[F:12][C:13]1[CH:14]=[CH:15][C:16]([NH:19][C:20]([C:22]2[C:26]([NH:27][C:5](=[O:7])[C:4]3[CH:8]=[CH:9][CH:10]=[CH:11][C:3]=3[O:2][CH3:1])=[CH:25][NH:24][N:23]=2)=[O:21])=[CH:17][CH:18]=1

참가 물질

6

반응물 4

HCID 111,2-DichloroethaneHCID 113702-Methoxybenzoic acidHCID 757711-HydroxybenzotriazoleHCID 178508056HCID 178508056, 화합물

생성물 1

HCID 1784895554-(2-Methoxy-benzoylamino)-1H-pyrazole-3-carboxylic acid (4-fluoro-phenyl)-amide수율 15%

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

2-Methoxy-benzoic acid (38 mg, 0.25 mmol) was added to a solution of 4-amino-1H-pyrazole-3-carboxylic acid (4-fluoro-phenyl)-amide (50 mg, 0.23 mmol), EDC (53 mg, 0.27 mmol), and HOBt (37 mg, 0.27 mmol) in DMF (5 ml). The reaction mixture was stirred at room temperature for 24 hours. The solvent was removed under reduced pressure. The residue was purified by preparative LC/MS and, after evaporation of product-containing fractions, yielded the product as a pinkish solid (12 mg, 15%). (LC/MS: Rt 4.00, [M+H]+ 354.67).

후처리

  1. customThe solvent was removed under reduced pressure
  2. customThe residue was purified by preparative LC/MS
  3. customafter evaporation of product-containing fractions

출처 및 근거

ORD 기록
ord-6574a4bb929d4bdcadd5d3a7a3ca1bb4
출처 데이터셋
uspto-grants-2014_07
특허 번호
US08779147B2

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