Trifluoroacetic acid → 1-[(4-Chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-(methoxy)methyl]cyclopropanecarboxylic acid

HRID 1475688노트

반응식

HRID 1475688 반응식
[Cl:1][C:2]1[CH:7]=[CH:6][C:5]([CH:8]([O:19][CH3:20])[C:9]2([C:12]([O:14]C(C)(C)C)=[O:13])[CH2:11][CH2:10]2)=[CH:4][C:3]=1[NH:21][C:22](=[O:37])[C@H:23]([C:30]1[CH:35]=[CH:34][C:33]([Cl:36])=[CH:32][CH:31]=1)[C@@H:24]([CH3:29])[C:25]([F:28])([F:27])[F:26].C(O)(C(F)(F)F)=O>ClCCl>[Cl:1][C:2]1[CH:7]=[CH:6][C:5]([CH:8]([O:19][CH3:20])[C:9]2([C:12]([OH:14])=[O:13])[CH2:10][CH2:11]2)=[CH:4][C:3]=1[NH:21][C:22](=[O:37])[C@H:23]([C:30]1[CH:31]=[CH:32][C:33]([Cl:36])=[CH:34][CH:35]=1)[C@@H:24]([CH3:29])[C:25]([F:28])([F:27])[F:26]

참가 물질

4

반응물 2

HCID 6422Trifluoroacetic acidHCID 68006868tert-butyl 1-[(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)(methoxy)methyl]cyclopropanecarboxylate

생성물 1

HCID 573444421-[(4-Chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-(methoxy)methyl]cyclopropanecarboxylic acid

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

151 mg (0.269 mmol) of tert-butyl 1-[(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)(methoxy)methyl]cyclopropanecarboxylate (as diastereomer mixture) were dissolved in 2.9 ml of dichloromethane, and 1.0 ml of TFA was added at RT. After 30 min at RT, the reaction mixture was concentrated under reduced pressure and the residue was concentrated under reduced pressure. The crude product obtained in this manner was purified by RP-HPLC (mobile phase acetonitrile/water). This gave 87 mg (64% of theory) of the target compound.

후처리

  1. concentrationthe reaction mixture was concentrated under reduced pressure
  2. concentrationthe residue was concentrated under reduced pressure

출처 및 근거

ORD 기록
ord-feef6a714b224708909cfd7a3c60f556
출처 데이터셋
uspto-grants-2015_04
특허 번호
US09018258B2

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