Trifluoroacetic acid → (6-{4-[6-(4-Fluoro-phenyl)-2-(2-(R)-methyl-pyrrolidin-1-yl)-pyrimidin-4-yl]-3-(R)-methyl-piperazin-1-yl}-5-methyl-pyridin-3-yl)-acetic acid

HRID 2195063노트

반응식

HRID 2195063 반응식
C([O:5][C:6](=[O:41])[CH2:7][C:8]1[CH:9]=[N:10][C:11]([N:15]2[CH2:20][CH2:19][N:18]([C:21]3[CH:26]=[C:25]([C:27]4[CH:32]=[CH:31][C:30]([F:33])=[CH:29][CH:28]=4)[N:24]=[C:23]([N:34]4[CH2:38][CH2:37][CH2:36][C@H:35]4[CH3:39])[N:22]=3)[C@H:17]([CH3:40])[CH2:16]2)=[C:12]([CH3:14])[CH:13]=1)(C)(C)C.C(O)(C(F)(F)F)=O>C(Cl)Cl>[F:33][C:30]1[CH:29]=[CH:28][C:27]([C:25]2[N:24]=[C:23]([N:34]3[CH2:38][CH2:37][CH2:36][C@H:35]3[CH3:39])[N:22]=[C:21]([N:18]3[CH2:19][CH2:20][N:15]([C:11]4[N:10]=[CH:9][C:8]([CH2:7][C:6]([OH:41])=[O:5])=[CH:13][C:12]=4[CH3:14])[CH2:16][C@H:17]3[CH3:40])[CH:26]=2)=[CH:32][CH:31]=1

참가 물질

4

반응물 2

HCID 6422Trifluoroacetic acidHCID 59168306(6-{4-[6-(4-Fluoro-phenyl)-2-(2-(R)-methyl-pyrrolidin-1-yl)-pyrimidin-4-yl]-3-(R)-methyl-piperazin-1-yl)-5-methyl-pyridin-3-yl)-acetic acid tert-butyl ester

생성물 1

HCID 59168364(6-{4-[6-(4-Fluoro-phenyl)-2-(2-(R)-methyl-pyrrolidin-1-yl)-pyrimidin-4-yl]-3-(R)-methyl-piperazin-1-yl}-5-methyl-pyridin-3-yl)-acetic acid

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

Stir a solution of (6-{4-[6-(4-fluoro-phenyl)-2-(2-(R)-methyl-pyrrolidin-1-yl)-pyrimidin-4-yl]-3-(R)-methyl-piperazin-1-yl}-5-methyl-pyridin-3-yl)-acetic acid tert-butyl ester (210 mg, 0.375 mmol) and 1 mL of TFA in DCM (10 mL) at room temperature for 16 h. Concentrate and partition between EtOAc and sat. NaHCO3. Dry the organic layer (Na2SO4) and concentrate under reduced pressure. Purify using flash chromatography eluting with MeOH-DCM (1:19) to give the title compound.

후처리

  1. concentrationConcentrate
  2. custompartition between EtOAc and sat. NaHCO3
  3. dry with materialDry the organic layer (Na2SO4)
  4. concentrationconcentrate under reduced pressure
  5. customPurify
  6. washeluting with MeOH-DCM (1:19)

출처 및 근거

ORD 기록
ord-c22cb871cb0542119eaa1f92dbead623
출처 데이터셋
uspto-grants-2012_12
특허 번호
US08334382B2

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