Dichloromethane → 3-[(4-Chlorophenyl)(cyclopropyl)methyl]-7-[(methylsulfinyl)methyl]-1H-indole

HRID 561667ノート

反応式

HRID 561667 の反応式
[Cl:1][C:2]1[CH:7]=[CH:6][C:5]([CH:8]([CH:21]2[CH2:23][CH2:22]2)[C:9]2[C:17]3[C:12](=[C:13]([CH2:18][S:19][CH3:20])[CH:14]=[CH:15][CH:16]=3)[NH:11][CH:10]=2)=[CH:4][CH:3]=1.ClCCl.ClC1C=CC=C(C(OO)=[O:35])C=1>CO>[Cl:1][C:2]1[CH:7]=[CH:6][C:5]([CH:8]([CH:21]2[CH2:23][CH2:22]2)[C:9]2[C:17]3[C:12](=[C:13]([CH2:18][S:19]([CH3:20])=[O:35])[CH:14]=[CH:15][CH:16]=3)[NH:11][CH:10]=2)=[CH:4][CH:3]=1

参加物

5

反応物 3

HCID 6344DichloromethaneHCID 70297m-Chloroperbenzoic acidHCID 583921383-[(4-Chlorophenyl)(cyclopropyl)methyl]-7-[(methylsulfanyl)methyl]-1H-indole

生成物 1

HCID 583922543-[(4-Chlorophenyl)(cyclopropyl)methyl]-7-[(methylsulfinyl)methyl]-1H-indole収率 130.1%

試薬・触媒・溶媒 1

HCID 887Methanol溶媒

実験手順

100 mg (0.29 mmol) of the compound from Example 227 were introduced into 15 ml of dichloromethane at 0° C., 72 mg (0.29 mmol) of 70% pure meta-chloroperbenzoic acid were added, and the mixture was stirred at RT for 2 h. 2 ml of methanol were added, and the solution was concentrated. The crude product was purified by preparative HPLC (mobile phase: acetonitrile/water gradient) to result in 135 mg of the title compound as mixture of diastereomers.

後処理

  1. concentrationthe solution was concentrated
  2. customThe crude product was purified by preparative HPLC (mobile phase: acetonitrile/water gradient)

出典と根拠

ORDレコード
ord-32d3d8266a0d4e83aa39823b0ab866ba
出典データセット
uspto-grants-2011_11
特許番号
US08063234B2

反応ノート

読み込み中…