Water → 5-Chloro-N-(3-{[3-fluoro-4-(3-oxo-4-morpholinyl)phenyl]amino}-2-hydroxypropyl)-2-thiophenecarboxamide

HRID 499736ノート

反応式

HRID 499736 の反応式
[NH2:1][C:2]1[CH:7]=[CH:6][C:5]([N:8]2[CH2:13][CH2:12][O:11][CH2:10][C:9]2=[O:14])=[C:4]([F:15])[CH:3]=1.[Cl:16][C:17]1[S:21][C:20]([C:22]([NH:24][CH2:25][CH:26]2[CH2:28][O:27]2)=[O:23])=[CH:19][CH:18]=1.O>C(O)C>[Cl:16][C:17]1[S:21][C:20]([C:22]([NH:24][CH2:25][CH:26]([OH:27])[CH2:28][NH:1][C:2]2[CH:7]=[CH:6][C:5]([N:8]3[CH2:13][CH2:12][O:11][CH2:10][C:9]3=[O:14])=[C:4]([F:15])[CH:3]=2)=[O:23])=[CH:19][CH:18]=1

参加物

5

反応物 3

HCID 962WaterHCID 219197985-chloro-N-(2-oxiranylmethyl)-2-thiophenecarboxamideHCID 231053114-(4-Amino-2-fluoro-phenyl)-morpholin-3-one

生成物 1

HCID 210707105-Chloro-N-(3-{[3-fluoro-4-(3-oxo-4-morpholinyl)phenyl]amino}-2-hydroxypropyl)-2-thiophenecarboxamide

試薬・触媒・溶媒 1

HCID 702Ethanol溶媒

実験手順

800 mg (3.8 mmol) of 4-(4-amino-2-fluorophenyl)-3-morpholinone and 700 mg (3.22 mmol) of 5-chloro-N-(2-oxiranylmethyl)-2-thiophenecarboxamide are heated in 15 ml of ethanol and 1 ml of water under reflux for 6 hours. The mixture is evaporated in vacuo, the crystals which have separated out after treatment with ethyl acetate are filtered off with suction, and chromatography of the mother liquor results in 276 mg (17% of theory) of the target compound.

後処理

  1. customThe mixture is evaporated in vacuo
  2. customthe crystals which have separated out after treatment with ethyl acetate
  3. filtrationare filtered off with suction, and chromatography of the mother liquor
  4. customresults in 276 mg (17% of theory) of the target compound

出典と根拠

ORDレコード
ord-23c0b1ef7eef4a439f61e36f51cb7ac1
出典データセット
uspto-grants-2010_08
特許番号
US07767702B2

反応ノート

読み込み中…