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

HRID 499736노트

반응식

HRID 499736 반응식
[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

참가 물질

5

반응물 3

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

생성물 1

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

시약·촉매·용매 1

HCID 702Ethanol용매

실험 절차

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.

후처리

  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

출처 및 근거

ORD 기록
ord-23c0b1ef7eef4a439f61e36f51cb7ac1
출처 데이터셋
uspto-grants-2010_08
특허 번호
US07767702B2

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