Morpholine → 2-Morpholin-4-yl-7-oxo-4,5,6,7-tetrahydro-benzo[b]thiophene-3-sulfonic acid[2-(4-fluorophenyl)-2-hydroxy-ethyl]-methyl-amide

HRID 1351285ノート

反応式

HRID 1351285 の反応式
[F:1][C:2]1[CH:7]=[CH:6][C:5]([CH:8]([OH:26])[CH2:9][N:10]([CH3:25])[S:11]([C:14]2[C:15]3[CH2:23][CH2:22][CH2:21][C:20](=[O:24])[C:16]=3[S:17][C:18]=2Br)(=[O:13])=[O:12])=[CH:4][CH:3]=1.[NH:27]1[CH2:32][CH2:31][O:30][CH2:29][CH2:28]1>C(N(CC)CC)C>[F:1][C:2]1[CH:7]=[CH:6][C:5]([CH:8]([OH:26])[CH2:9][N:10]([CH3:25])[S:11]([C:14]2[C:15]3[CH2:23][CH2:22][CH2:21][C:20](=[O:24])[C:16]=3[S:17][C:18]=2[N:27]2[CH2:32][CH2:31][O:30][CH2:29][CH2:28]2)(=[O:13])=[O:12])=[CH:4][CH:3]=1

参加物

4

反応物 2

HCID 8083MorpholineHCID 210985782-Bromo-7-oxo-4,5,6,7-tetrahydro-benzo[b]thiophene-3-sulfonic acid [2-(4-fluorophenyl)-2-hydroxy-ethyl]-methyl-amide

生成物 1

HCID 210985882-Morpholin-4-yl-7-oxo-4,5,6,7-tetrahydro-benzo[b]thiophene-3-sulfonic acid[2-(4-fluorophenyl)-2-hydroxy-ethyl]-methyl-amide

試薬・触媒・溶媒 1

HCID 8471Triethylamine溶媒

反応条件

温度
60 °C

実験手順

2-Bromo-7-oxo-4,5,6,7-tetrahydro-benzo[b]thiophene-3-sulfonic acid[2-(4-fluorophenyl)-2-hydroxy-ethyl]-methyl-amide (the compound of Preparation Example 58) (80 mg), triethylamine (29 mL) and morpholin (24 μL) were stirred at 60° C. for 3 hours. The residue resulting from the evaporation of the solvent at reduced pressure was purified by silica gel column chromatography (hexane/ethyl acetate), and the title compound (82 mg) was obtained as a colorless candy-like substance.

後処理

  1. customThe residue resulting from the evaporation of the solvent at reduced pressure
  2. customwas purified by silica gel column chromatography (hexane/ethyl acetate)

出典と根拠

ORDレコード
ord-fe4d297eaac5407bb8bfbe75b9f2da3d
出典データセット
uspto-grants-2007_05
特許番号
US07217723B2

反応ノート

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