反応 #7515

ord-a61417b4a55b431fb3b5c4a7891ca0c1

反応方程式

O
water
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1Cl
ethyl 4-chloro-2-(2,3-dihydro-1H-indol-1-yl)-5-pyrimidinecarboxylate
O=C([O-])[O-].[Na+].[Na+]
sodium carbonate
NCc1ccc(F)cc1
4-fluorobenzylamine
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1NCc1ccc(F)cc1
title compound
収率 81.2%
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1NCc1ccc(F)cc1
ethyl 2-(2,3-dihydro-1H-indol-1-yl)-4-[(4-fluorobenzyl)amino]-5-pyrimidinecarboxylate
収率 81.2%

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    温度the mixture was heated
  2. 2
    温度under reflux for 18 h
  3. 3
    ろ過The precipitated crystals were collected by filtration
  4. 4
    洗浄washed several times with cold water and cold ether
  5. 5
    その他dried

実験手順

To a solution of ethyl 4-chloro-2-(2,3-dihydro-1H-indol-1-yl)-5-pyrimidinecarboxylate (607 mg, 2.0 mmol) in isopropanol (5 mL) were added sodium carbonate (424 mg, 4 mmol) and 4-fluorobenzylamine (313 mg, 4 mmol) and the mixture was heated under reflux for 18 h. The reaction mixture was allowed to cool to room temperature and water was added. The precipitated crystals were collected by filtration, washed several times with cold water and cold ether and dried to give the title compound (637 mg, 81%).

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US07087597B1uspto-grants-2006_08