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2,6-Dimethylmorpholine, cis- → N-{6-Bromo-1-[(4-methylphenyl)sulfonyl]-1H-indazol-4-yl}-2-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-thiazole-4-carboxamide

HRID 1695738
ノート
印刷プレビュー

反応式

HRID 1695738 の反応式
[CH3:1][C@H:2]1[O:7][C@@H:6]([CH3:8])[CH2:5][NH:4][CH2:3]1.[Br:9][C:10]1[CH:18]=[C:17]2[C:13]([CH:14]=[N:15][N:16]2[S:19]([C:22]2[CH:27]=[CH:26][C:25]([CH3:28])=[CH:24][CH:23]=2)(=[O:21])=[O:20])=[C:12]([NH:29][C:30]([C:32]2[N:33]=[C:34]([CH2:37]Cl)[S:35][CH:36]=2)=[O:31])[CH:11]=1>C(#N)C>[Br:9][C:10]1[CH:18]=[C:17]2[C:13]([CH:14]=[N:15][N:16]2[S:19]([C:22]2[CH:27]=[CH:26][C:25]([CH3:28])=[CH:24][CH:23]=2)(=[O:21])=[O:20])=[C:12]([NH:29][C:30]([C:32]2[N:33]=[C:34]([CH2:37][N:4]3[CH2:5][C@H:6]([CH3:8])[O:7][C@H:2]([CH3:1])[CH2:3]3)[S:35][CH:36]=2)=[O:31])[CH:11]=1
参加物実験手順後処理出典と根拠反応ノート

参加物

4

反応物 2

HCID 6415002,6-Dimethylmorpholine, cis-HCID 58255773N-{6-Bromo-1-[(4-methylphenyl)sulfonyl]-1H-indazol-4-yl}-2-(chloromethyl)-1,3-thiazole-4-carboxamide

生成物 1

HCID 58255797N-{6-Bromo-1-[(4-methylphenyl)sulfonyl]-1H-indazol-4-yl}-2-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-thiazole-4-carboxamide

試薬・触媒・溶媒 1

HCID 6342Acetonitrile溶媒

実験手順

Acetonitrile (15 mL) and (2R,6S)-2,6-dimethylmorpholine (1.4 ml) were added to N-{6-bromo-1-[(4-methylphenyl)sulfonyl]-1H-indazol-4-yl}-2-(chloromethyl)-1,3-thiazole-4-carboxamide (2 g) and the reaction mixture was refluxed for 3 h. On cooling a solid precipitated. The mixture was diluted with acetonitrile (15 ml) and the solid was collected by filtration, washing with acetonitrile. The solid was dried on the vacuum pump overnight to give title compound (1.86 g).

後処理

  1. temperaturethe reaction mixture was refluxed for 3 h
  2. temperatureOn cooling a solid
  3. customprecipitated
  4. additionThe mixture was diluted with acetonitrile (15 ml)
  5. filtrationthe solid was collected by filtration
  6. washwashing with acetonitrile
  7. customThe solid was dried on the vacuum

出典と根拠

ORDレコード
ord-55b25909ccc740d9bfcccb23b84fbbf1
出典データセット
uspto-grants-2012_04
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US08163743B2

反応ノート

読み込み中…

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