7-Chloro-benzo[1,4]dioxin-2-one → 2-(4-Chloro-2-hydroxy-phenoxy)-1-[4-(4-fluoro-benzyl)-(2R)-2-methyl-piperazin-1-yl]-ethanone

HRID 11722

反応式

HRID 11722 の反応式
[Cl:1][C:2]1[CH:3]=[CH:4][C:5]2[O:10][CH2:9][C:8](=[O:11])[O:7][C:6]=2[CH:12]=1.[F:13][C:14]1[CH:27]=[CH:26][C:17]([CH2:18][N:19]2[CH2:24][CH2:23][NH:22][C@H:21]([CH3:25])[CH2:20]2)=[CH:16][CH:15]=1>C1(C)C=CC=CC=1>[Cl:1][C:2]1[CH:3]=[CH:4][C:5]([O:10][CH2:9][C:8]([N:22]2[CH2:23][CH2:24][N:19]([CH2:18][C:17]3[CH:26]=[CH:27][C:14]([F:13])=[CH:15][CH:16]=3)[CH2:20][C@H:21]2[CH3:25])=[O:11])=[C:6]([OH:7])[CH:12]=1

参加物

4

反応物 2

HCID 32553187-Chloro-benzo[1,4]dioxin-2-oneHCID 11600914(r)-1-(4-Fluorobenzyl)-3-methylpiperazine

生成物 1

HCID 696558562-(4-Chloro-2-hydroxy-phenoxy)-1-[4-(4-fluoro-benzyl)-(2R)-2-methyl-piperazin-1-yl]-ethanone収率 52.9%

試薬・触媒・溶媒 1

HCID 1140Toluene溶媒

反応条件

温度
95 °C

実験手順

To a solution of 7-chloro-benzo[1,4]dioxin-2-one (0.845 g, 4.81 mmol) in toluene (25 mL) was added (3R)-1-(4-fluoro-benzyl)-3-methyl-piperazine (1.003 g, 4.81 mmol). The resulting mixture was heated to 95° C. overnight. The reaction was cooled to ambient temperature, filtered and concentrated in vacuo. Chromatography on silica gel gave the title compound (˜1 g).

後処理

  1. temperatureThe reaction was cooled to ambient temperature
  2. filtrationfiltered
  3. concentrationconcentrated in vacuo

出典と根拠

ORDレコード
ord-6326dfff423e40298d12cdfe41a6ac19
出典データセット
uspto-grants-2006_08
特許番号
US07098212B2

関連ノート

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