4-Methylmorpholine → N-(2-fluoro-4-chloro-5-cyclopentyloxyphenyl)-N'-(4-fluorocumyl)-3,4,5,6-tetrahydrophthalamide

HRID 1720418ノート

反応式

HRID 1720418 の反応式
[F:1][C:2]1[CH:7]=[C:6]([Cl:8])[C:5]([O:9][CH:10]2[CH2:14][CH2:13][CH2:12][CH2:11]2)=[CH:4][C:3]=1[N:15]1C(=O)C2CCCC(=C2)[C:16]1=[O:25].[F:26][C:27]1[CH:36]=[CH:35][C:30]([C:31]([NH2:34])([CH3:33])[CH3:32])=[CH:29][CH:28]=1.CN1[CH2:43][CH2:42][O:41]CC1>C1C=CC=CC=1>[F:1][C:2]1[CH:7]=[C:6]([Cl:8])[C:5]([O:9][CH:10]2[CH2:14][CH2:13][CH2:12][CH2:11]2)=[CH:4][C:3]=1[NH:15][C:16](=[O:25])[C:6]1[CH2:7][CH2:2][CH2:3][CH2:4][C:43]=1[C:42]([NH:34][C:31]([C:30]1[CH:29]=[CH:28][C:27]([F:26])=[CH:36][CH:35]=1)([CH3:33])[CH3:32])=[O:41]

参加物

5

反応物 3

HCID 79724-MethylmorpholineHCID 130256651-(4-Fluorophenyl)-1-methylethylamineHCID 19425191N-(2-fluoro-4-chloro-5-cyclopentyloxyphenyl)-3,4,5,6-tetrahydroisophthalimide

生成物 1

HCID 22417586N-(2-fluoro-4-chloro-5-cyclopentyloxyphenyl)-N'-(4-fluorocumyl)-3,4,5,6-tetrahydrophthalamide収率 58.7%

試薬・触媒・溶媒 1

HCID 241Benzene溶媒

実験手順

N-(2-Fluoro-4-chloro-5-cyclopentyloxyphenyl)-3,4,5,6-tetrahydroisophthalimide (1.00 g, 2.75 mmol), 4-fluorocumylamine (0.600 g, 3.92 mmol), N-methylmorpholine (0.330 g, 3.26 mmol), and benzene (10 ml) as a solvent were placed into a round bottom flask (50 cc) and stirred overnight at room temperature. After completion of the reaction, the solvent was distilled off under reduced pressure, and the resulting crude product was recrystallized from ethyl acetate/acetone to obtain N-(2-fluoro-4-chloro-5-cyclopentyloxyphenyl)-N'-(4-fluorocumyl)-3,4,5,6-tetrahydrophthalamide as white crystals (0.417 g, 29.3% yield).

後処理

  1. customAfter completion of the reaction
  2. distillationthe solvent was distilled off under reduced pressure
  3. customthe resulting crude product was recrystallized from ethyl acetate/acetone

出典と根拠

ORDレコード
ord-afd427aa053d4873b0ffa2685dd89f3f
出典データセット
uspto-grants-1996_04
特許番号
US05506190

反応ノート

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