Maleic Anhydride → (1S)-2-(1-Cyclohexylpiperidin-4-yl)-1-methyl-3-oxo-2,3-dihydro-1H-isoindole-4-carboxylic acid

HRID 1618115ノート

反応式

HRID 1618115 の反応式
[CH:1]1([N:7]2[CH2:12][CH2:11][CH:10]([NH:13][C@H:14]([C:16]3O[CH:18]=[CH:19][CH:20]=3)[CH3:15])[CH2:9][CH2:8]2)[CH2:6][CH2:5][CH2:4][CH2:3][CH2:2]1.[C:21]1(=[O:27])[O:26][C:24](=[O:25])[CH:23]=[CH:22]1>C1(C)C=CC=CC=1>[CH:1]1([N:7]2[CH2:8][CH2:9][CH:10]([N:13]3[C:24](=[O:25])[C:23]4[C:22]([C:21]([OH:26])=[O:27])=[CH:18][CH:19]=[CH:20][C:16]=4[C@@H:14]3[CH3:15])[CH2:11][CH2:12]2)[CH2:6][CH2:5][CH2:4][CH2:3][CH2:2]1

参加物

4

反応物 2

HCID 7923Maleic AnhydrideHCID 671921261-cyclohexyl-N-[(1S)-1-(furan-2-yl)ethyl]piperidin-4-amine

生成物 1

HCID 67191867(1S)-2-(1-Cyclohexylpiperidin-4-yl)-1-methyl-3-oxo-2,3-dihydro-1H-isoindole-4-carboxylic acid

試薬・触媒・溶媒 1

HCID 1140Toluene溶媒

反応条件

温度
100 °C

実験手順

1-Cyclohexyl-N-[(1S)-1-(furan-2-yl)ethyl]piperidin-4-amine (0.3 gr, 1.08 mmol) and maleic anhydride (0.13 gr, 1.3 mmol) in toluene (10 mL) were stirred at reflux for 16 hours. Solvent was evaporated and the residue was dissolved in aqueous 37% hydrochloric acid (5 mL) and stirred at 100° C. for 2 hours. Volatiles were evaporated affording crude title product that was used for the next step without further purification

後処理

  1. temperatureat reflux for 16 hours
  2. customSolvent was evaporated
  3. dissolutionthe residue was dissolved in aqueous 37% hydrochloric acid (5 mL)
  4. customVolatiles were evaporated

出典と根拠

ORDレコード
ord-f579d8ef94394998baa2c9e63caaeb02
出典データセット
uspto-grants-2014_07
特許番号
US08765972B2

反応ノート

読み込み中…