Trifluoroacetic acid → 3-[(4-Chloro-2,6-difluorophenyl)(cyclopropyl)methyl]-7-[(methylsulfanyl)methyl]-1H-indole

HRID 561662노트

반응식

HRID 561662 반응식
[Cl:1][C:2]1[CH:7]=[C:6]([F:8])[C:5]([CH:9]([CH:11]2[CH2:13][CH2:12]2)O)=[C:4]([F:14])[CH:3]=1.FC(F)(F)C(O)=O.[CH3:22][S:23][CH2:24][C:25]1[CH:26]=[CH:27][CH:28]=[C:29]2[C:33]=1[NH:32][CH:31]=[CH:30]2>ClCCl>[Cl:1][C:2]1[CH:7]=[C:6]([F:8])[C:5]([CH:9]([CH:11]2[CH2:13][CH2:12]2)[C:30]2[C:29]3[C:33](=[C:25]([CH2:24][S:23][CH3:22])[CH:26]=[CH:27][CH:28]=3)[NH:32][CH:31]=2)=[C:4]([F:14])[CH:3]=1

참가 물질

5

반응물 3

HCID 6422Trifluoroacetic acidHCID 583921877-[(Methylsulfanyl)methyl]-1H-indoleHCID 58392245(4-Chloro-2,6-difluorophenyl)(cyclopropyl)methanol

생성물 1

HCID 583922883-[(4-Chloro-2,6-difluorophenyl)(cyclopropyl)methyl]-7-[(methylsulfanyl)methyl]-1H-indole

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

617 mg (2.82 mmol) of the compound from Example 156A and 0.26 ml (3.39 mmol) of trifluoroacetic acid were added to 500 mg (2.82 mmol) of the compound from Example 8A in 20 ml of dichloromethane. The reaction mixture was stirred at RT overnight, the solvent was removed in vacuo, and the crude product was then purified by preparative HPLC (mobile phase: acetonitrile/water gradient). 155 mg (14% 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-f33acc5dbe9a46fd8466c1820951842d
출처 데이터셋
uspto-grants-2011_11
특허 번호
US08063234B2

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