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

HRID 561659ノート

反応式

HRID 561659 の反応式
[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.[CH3:20][S:21][CH2:22][C:23]1[CH:24]=[CH:25][CH:26]=[C:27]2[C:31]=1[NH:30][CH:29]=[CH:28]2>ClCCl>[Cl:12][C:9]1[CH:10]=[CH:11][C:6]([CH:4]([CH:1]2[CH2:3][CH2:2]2)[C:28]2[C:27]3[C:31](=[C:23]([CH2:22][S:21][CH3:20])[CH:24]=[CH:25][CH:26]=3)[NH:30][CH:29]=2)=[CH:7][CH:8]=1

参加物

5

反応物 3

HCID 6422Trifluoroacetic acidHCID 866794-Chloro-alpha-cyclopropylbenzenemethanolHCID 583921877-[(Methylsulfanyl)methyl]-1H-indole

生成物 1

HCID 583921383-[(4-Chlorophenyl)(cyclopropyl)methyl]-7-[(methylsulfanyl)methyl]-1H-indole

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

515 mg (2.82 mmol) of the compound from Example 153A 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 for 30 min, the solvent was removed in vacuo, and the crude product was then purified by preparative HPLC (mobile phase: acetonitrile/water gradient). 500 mg (50% of theory) of the title compound were obtained.

後処理

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

出典と根拠

ORDレコード
ord-030c8b85c683487d97e7218ce10012af
出典データセット
uspto-grants-2011_11
特許番号
US08063234B2

反応ノート

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