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Water → 3-{[2-Fluoro-1-(fluoromethyl)ethyl]oxy}-5-[(9-fluoro-4-methyl-5-oxo-2,3,4,5-tetrahydro-1,4-benzoxazepin-8-yl)oxy]-n-(1-methyl-1h-pyrazol-3-yl)benzamide

HRID 548682
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HRID 548682 반응식
[F:1][CH2:2][CH:3]([O:6][C:7]1[CH:8]=[C:9]([CH:19]=[C:20]([OH:22])[CH:21]=1)[C:10]([NH:12][C:13]1[CH:17]=[CH:16][N:15]([CH3:18])[N:14]=1)=[O:11])[CH2:4][F:5].CC([Si](C)(C)[O:28][CH2:29][CH2:30][N:31]([CH3:43])[C:32](=[O:42])[C:33]1[CH:38]=[CH:37][C:36](F)=[C:35]([F:40])[C:34]=1F)(C)C.C(=O)([O-])[O-].[K+].[K+].O>CC(N(C)C)=O>[F:5][CH2:4][CH:3]([O:6][C:7]1[CH:8]=[C:9]([CH:19]=[C:20]([O:22][C:36]2[CH:37]=[CH:38][C:33]3[C:32](=[O:42])[N:31]([CH3:43])[CH2:30][CH2:29][O:28][C:34]=3[C:35]=2[F:40])[CH:21]=1)[C:10]([NH:12][C:13]1[CH:17]=[CH:16][N:15]([CH3:18])[N:14]=1)=[O:11])[CH2:2][F:1]
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참가 물질

6

반응물 4

HCID 962WaterHCID 11430Potassium CarbonateHCID 57663171N-(2-{[(1,1-Dimethylethyl)(dimethyl)silyl]oxy}ethyl)-2,3,4-trifluoro-N-methylbenzamideHCID 591271643-{[2-fluoro-1-(fluoromethyl)ethyl]oxy}-5-hydroxy-N-(1-methyl-1H-pyrazol-3-yl)benzamide

생성물 1

HCID 159494053-{[2-Fluoro-1-(fluoromethyl)ethyl]oxy}-5-[(9-fluoro-4-methyl-5-oxo-2,3,4,5-tetrahydro-1,4-benzoxazepin-8-yl)oxy]-n-(1-methyl-1h-pyrazol-3-yl)benzamide
수율 3.1%

시약·촉매·용매 1

HCID 31374Dimethylacetamide용매

실험 절차

A solution of 3-{[2-fluoro-1-(fluoromethyl)ethyl]oxy}-5-hydroxy-N-(1-methyl-1H-pyrazol-3-yl)benzamide (100 mg, 0.32 mmol), N-(2-{[(1,1-dimethylethyl)(dimethyl)silyl]oxy}ethyl)-2,3,4-trifluoro-N-methylbenzamide (112 mg, 0.32 mmol) and potassium carbonate (89 mg, 0.64 mmol) in DMA (2 mL) was heated in a microwave reactor for 2 hours. Water (20 mL) was added and the solution extracted with ethyl acetate. The ethyl acetate layer was washed with brine (20 mL), dried (MgSO4) and evaporated to a residue which was taken up in DCM (10 mL) and TFA (5 drops) added. The mixture was stirred at RT for 2 hours. The solvent was evaporated to a residue, which was chromatographed by preparative HPLC on C18 reversed phase, eluting with 5-95% acetonitrile (+0.2% TFA) in water (+0.2% TFA), to give the required product (5 mg).

후처리

  1. extractionthe solution extracted with ethyl acetate
  2. washThe ethyl acetate layer was washed with brine (20 mL)
  3. dry with materialdried (MgSO4)
  4. customevaporated to a residue which
  5. additionTFA (5 drops) added
  6. customThe solvent was evaporated to a residue, which
  7. customwas chromatographed by preparative HPLC on C18 reversed phase
  8. washeluting with 5-95% acetonitrile (+0.2% TFA) in water (+0.2% TFA)

출처 및 근거

ORD 기록
ord-5c476d9a34f5470b9fd75eff910976dd
출처 데이터셋
uspto-grants-2011_05
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US07943607B2

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