反応 #80221

ord-33a7c14d4bd14e5f948fd44a914e6cd8

反応方程式

On1nnc2ccccc21
1-hydroxybenzotriazole
O=C(O)c1cnc2cc(NC(=O)c3ccccc3-c3ccc(C(F)(F)F)cc3)ccc2c1
7-[(4′-Trifluoromethyl-biphenyl-2-carbonyl)-amino]-quinoline-3-carboxylic acid
NCc1ccc(F)cc1
4-fluorobenzylamine
CCN(CC)CC
triethylamine
CCN=C=NCCCN(C)C.Cl
1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride
O=C(NCc1ccc(F)cc1)c1cnc2cc(NC(=O)c3ccccc3-c3ccc(C(F)(F)F)cc3)ccc2c1
title compound
収率 76.8%
O=C(NCc1ccc(F)cc1)c1cnc2cc(NC(=O)c3ccccc3-c3ccc(C(F)(F)F)cc3)ccc2c1
7-[(4′-Trifluoromethyl-biphenyl-2-carbonyl)-amino]-quinoline-3-carboxylic acid 4-fluoro-benzylamide
収率 76.8%

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    濃縮the reaction mixture was concentrated
  2. 2
    ろ過the solid was collected by vacuum filtration

実験手順

7-[(4′-Trifluoromethyl-biphenyl-2-carbonyl)-amino]-quinoline-3-carboxylic acid (100 mg, 0.23 mmol) was combined with 4-fluorobenzylamine (34 mg, 0.27 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (53 mg, 0.27 mmol), 1-hydroxybenzotriazole (34 mg, 0.25 mmol), and triethylamine (0.13 ml, 0.92 mmol) in 1.5 ml of dichloromethane. After stirring overnight at ambient temperature, the reaction mixture was concentrated, the residue was suspended in water, and the solid was collected by vacuum filtration to afford 96 mg of the title compound as a colorless solid.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US06713489B2uspto-grants-2004_03