Trifluoroacetic acid → 3-[(4-Chlorophenyl)(cyclopropyl)methyl]-5-fluoro-7-[(methylsulfonyl)methyl]-1H-indole

HRID 561675노트

반응식

HRID 561675 반응식
[CH:1]1([CH:4]([C:6]2[CH:11]=[CH:10][C:9]([Cl:12])=[CH:8][CH:7]=2)O)[CH2:3][CH2:2]1.FC(F)(F)C(O)=O.[F:20][C:21]1[CH:22]=[C:23]2[C:27](=[C:28]([CH2:30][S:31]([CH3:34])(=[O:33])=[O:32])[CH:29]=1)[NH:26][CH:25]=[CH:24]2>ClCCl>[Cl:12][C:9]1[CH:10]=[CH:11][C:6]([CH:4]([CH:1]2[CH2:3][CH2:2]2)[C:24]2[C:23]3[C:27](=[C:28]([CH2:30][S:31]([CH3:34])(=[O:32])=[O:33])[CH:29]=[C:21]([F:20])[CH:22]=3)[NH:26][CH:25]=2)=[CH:7][CH:8]=1

참가 물질

5

반응물 3

HCID 6422Trifluoroacetic acidHCID 866794-Chloro-alpha-cyclopropylbenzenemethanolHCID 583923185-Fluoro-7-[(methylsulfonyl)methyl]-1H-indole

생성물 1

HCID 583922023-[(4-Chlorophenyl)(cyclopropyl)methyl]-5-fluoro-7-[(methylsulfonyl)methyl]-1H-indole

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

64 mg (0.35 mmol) of the compound from Example 153A and 0.03 ml (0.42 mmol) of trifluoroacetic acid were added to 80 mg (0.35 mmol) of the compound from Example 87A in 2.5 ml of dichloromethane. The reaction mixture was stirred at RT for 45 min, the solvent was removed in vacuo, and the crude product was then purified by preparative HPLC (mobile phase: acetonitrile/water gradient). 110 mg (80% of theory) of the title compound were obtained.

후처리

  1. customthe solvent was removed in vacuo
  2. customthe crude product was then purified by preparative HPLC (mobile phase: acetonitrile/water gradient)

출처 및 근거

ORD 기록
ord-7f26d019e75b41eca4de21487de82cf5
출처 데이터셋
uspto-grants-2011_11
특허 번호
US08063234B2

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