Trifluoroacetic acid → 2-methyl-2-({4-[2-({1-[3-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl}oxy)ethyl]-1,3-thiazol-2-yl}thio)propionic acid

HRID 914345노트

반응식

HRID 914345 반응식
C([O:5][C:6](=[O:34])[C:7]([CH3:33])([S:9][C:10]1[S:11][CH:12]=[C:13]([CH2:15][CH2:16][O:17][C:18]2[CH:19]=[N:20][N:21]([C:23]3[CH:28]=[CH:27][CH:26]=[C:25]([C:29]([F:32])([F:31])[F:30])[CH:24]=3)[CH:22]=2)[N:14]=1)[CH3:8])(C)(C)C.FC(F)(F)C(O)=O>ClCCl>[CH3:33][C:7]([S:9][C:10]1[S:11][CH:12]=[C:13]([CH2:15][CH2:16][O:17][C:18]2[CH:19]=[N:20][N:21]([C:23]3[CH:28]=[CH:27][CH:26]=[C:25]([C:29]([F:32])([F:30])[F:31])[CH:24]=3)[CH:22]=2)[N:14]=1)([CH3:8])[C:6]([OH:34])=[O:5]

참가 물질

4

반응물 2

HCID 6422Trifluoroacetic acidHCID 597588922-methyl-2-({4-[2-({1-[3-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl}oxy)ethyl]-1,3-thiazol-2-yl}thio)propionic acid tert-butyl ester

생성물 1

HCID 597592522-methyl-2-({4-[2-({1-[3-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl}oxy)ethyl]-1,3-thiazol-2-yl}thio)propionic acid수율 81.4%

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

2-Methyl-2-({4-[2-({1-[3-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl}oxy)ethyl]-1,3-thiazol-2-yl}thio)propionic acid tert-butyl ester (400 mg) obtained in Example 158-1 was dissolved in dichloromethane (6 mL), trifluoroacetic acid (2 mL) was added, and the mixture was stirred at room temperature for 12 hr. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel chromatography (elution solvent; hexane:ethyl acetate=1:1 to 0:1) to give the title compound (290 mg) as a colorless oil.

후처리

  1. concentrationThe reaction mixture was concentrated under reduced pressure
  2. customthe residue was purified by silica gel chromatography (elution solvent; hexane:ethyl acetate=1:1 to 0:1)

출처 및 근거

ORD 기록
ord-9b48129e1cc3460e97563e4c65b3de9e
출처 데이터셋
uspto-grants-2011_09
특허 번호
US08026370B2

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