1,2-Diaminocyclohexane, trans- → 1-(3-Chloro-2-fluoro-phenyl)-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-one

HRID 80113

反応式

HRID 80113 の反応式
[CH3:1][C:2]1[CH:7]=[CH:6][N:5]=[CH:4][C:3]=1[N:8]1[CH2:12][CH2:11][NH:10][C:9]1=[O:13].Br[C:15]1[CH:20]=[CH:19][CH:18]=[C:17]([Cl:21])[C:16]=1[F:22].N[C@@H]1CCCC[C@H]1N.P([O-])([O-])([O-])=O.[K+].[K+].[K+]>[Cu](I)I.O1CCOCC1>[Cl:21][C:17]1[C:16]([F:22])=[C:15]([N:10]2[CH2:11][CH2:12][N:8]([C:3]3[CH:4]=[N:5][CH:6]=[CH:7][C:2]=3[CH3:1])[C:9]2=[O:13])[CH:20]=[CH:19][CH:18]=1

参加物

7

反応物 4

HCID 438061,2-Diaminocyclohexane, trans-HCID 62657Potassium Phosphate, TribasicHCID 36857621-Bromo-3-chloro-2-fluorobenzeneHCID 596361701-(4-Methylpyridin-3-yl)imidazolidin-2-one

生成物 1

HCID 596362041-(3-Chloro-2-fluoro-phenyl)-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-one収率 3.1%

試薬・触媒・溶媒 2

HCID 83717Copper iodide触媒HCID 312751,4-Dioxane溶媒

実験手順

Using the same reaction conditions as described in Example 14, 1-(4-methyl-pyridin-3-yl)-imidazolidin-2-one (I-14b: 0.15 g, 0.847 mmol) was reacted with 1-bromo-3-chloro-2-fluoro-benzene (0.211 g, 1.016 mmol), 1,4-dioxane (20 mL), copper iodide (0.015 g, 0.084 mmol), trans-1,2-diamino cyclohexane (0.028 g, 0.254 mmol) and potassium phosphate (0.445 g, 2.1 mmol) to afford 8 mg of the product (0.03% yield).

後処理

  1. customthe same reaction conditions

出典と根拠

ORDレコード
ord-44f99ce1a01046da91ca7db21ce6fc8b
出典データセット
uspto-grants-2014_09
特許番号
USRE045173E1

関連ノート

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