Trifluoroacetic acid → 3-[1-(1,3-Benzodioxol-5-yl)-1-cyclopropylethyl]-7-[(methylsulfanyl)methyl]-1H-indole

HRID 561639ノート

反応式

HRID 561639 の反応式
[O:1]1[C:5]2[CH:6]=[CH:7][C:8]([C:10]([CH:13]3[CH2:15][CH2:14]3)(O)[CH3:11])=[CH:9][C:4]=2[O:3][CH2:2]1.FC(F)(F)C(O)=O.[CH3:23][S:24][CH2:25][C:26]1[CH:27]=[CH:28][CH:29]=[C:30]2[C:34]=1[NH:33][CH:32]=[CH:31]2>ClCCl>[O:1]1[C:5]2[CH:6]=[CH:7][C:8]([C:10]([C:31]3[C:30]4[C:34](=[C:26]([CH2:25][S:24][CH3:23])[CH:27]=[CH:28][CH:29]=4)[NH:33][CH:32]=3)([CH:13]3[CH2:15][CH2:14]3)[CH3:11])=[CH:9][C:4]=2[O:3][CH2:2]1

参加物

5

反応物 3

HCID 6422Trifluoroacetic acidHCID 583921877-[(Methylsulfanyl)methyl]-1H-indoleHCID 583922611-(Benzo[d][1,3]dioxol-5-yl)-1-cyclopropylethanol

生成物 1

HCID 583921043-[1-(1,3-Benzodioxol-5-yl)-1-cyclopropylethyl]-7-[(methylsulfanyl)methyl]-1H-indole

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

600 mg (2.91 mmol) of the compound from Example 143A and 0.27 ml (3.49 mmol) of trifluoroacetic acid were added to 516 mg (2.91 mmol) of the compound from Example 8A in 4 ml of dichloromethane. The reaction mixture was stirred at RT for 30 min, and the crude product was then purified twice by preparative HPLC (mobile phase: acetonitrile/water gradient). 377 mg (35% of theory) of the title compound were obtained.

後処理

  1. customthe crude product was then purified twice by preparative HPLC (mobile phase: acetonitrile/water gradient)

出典と根拠

ORDレコード
ord-b39efd6c2e4c453c85a7af5b4ce8b073
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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