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Imidazole → 1-{3-(4-Fluorophenyl)-trans-3-[6-(4-fluorophenoxymethyl)tetrahydropyran-2-yloxy]propyl}imidazole

HRID 905086
ノート
印刷プレビュー

反応式

HRID 905086 の反応式
[NH:1]1[CH:5]=[CH:4][N:3]=[CH:2]1.[H-].[Na+].[F:8][C:9]1[CH:34]=[CH:33][C:12]([O:13][CH2:14][C@@H:15]2[O:20][C@@H:19]([O:21][CH:22]([C:26]3[CH:31]=[CH:30][C:29]([F:32])=[CH:28][CH:27]=3)[CH2:23][CH2:24]Cl)[CH2:18][CH2:17][CH2:16]2)=[CH:11][CH:10]=1>CN(C)C=O>[F:32][C:29]1[CH:28]=[CH:27][C:26]([CH:22]([O:21][C@H:19]2[CH2:18][CH2:17][CH2:16][C@H:15]([CH2:14][O:13][C:12]3[CH:33]=[CH:34][C:9]([F:8])=[CH:10][CH:11]=3)[O:20]2)[CH2:23][CH2:24][N:1]2[CH:5]=[CH:4][N:3]=[CH:2]2)=[CH:31][CH:30]=1
参加物実験手順後処理出典と根拠反応ノート

参加物

5

反応物 3

HCID 795ImidazoleHCID 24758Sodium hydrideHCID 54428102Trans-6-(4-fluorophenoxymethyl)-2-[3-chloro-1-(4-fluorophenyl)propoxy]tetrahydropyran

生成物 1

HCID 543473471-{3-(4-Fluorophenyl)-trans-3-[6-(4-fluorophenoxymethyl)tetrahydropyran-2-yloxy]propyl}imidazole収率 46.7%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide
溶媒
2 回

実験手順

A mixture of 56 mg of imidazole and 36 mg of 55% sodium hydride was stirred in 2 ml of dimethylformamide at 60°-70° C. for 30 minutes. The mixture was left to cool at room temperature, and then a solution of 218 mg of trans-6-(4-fluorophenoxymethyl)-2-[3-chloro-1-(4-fluorophenyl)propoxy]tetrahydropyran in 1 ml of dimethylformamide was added, and the mixture was heated, with stirring, at 80°-90° C. for 6 hours. At the end of this time, the mixture was treated and the product purified essentially as described in Example 34(b)(i), to give 110 mg of the title compound.

後処理

  1. waitThe mixture was left
  2. temperaturethe mixture was heated
  3. additionAt the end of this time, the mixture was treated
  4. customthe product purified essentially

出典と根拠

ORDレコード
ord-f312534bff594adfa4a10f5d0d3d3a98
出典データセット
uspto-grants-1983_12
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US04421758

反応ノート

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