反应详情

To a suspension of 4-[4-[[7-(trifluoromethyl)-4-quinolinyl]amino]benzoyl]piperazine (2 g, 0.005 mol) in 15 ml of methylene chloride is added dropwise a solution of p-tolyl isocyanate in 10 ml of methylene chloride under nitrogen at room temperature. After complete addition, the resultant suspension is stirred at room temperature for 2 hours. This suspension is then filtered and the white residue is washed with methylene chloride and dried. This is re-crystallized from methanol/methylene chloride to give 2.5 g (93%) of white crystalline 1-[[(4-methylphenyl)amino]carbonyl]-4-[4-[[7-(trifluoromethyl)-4-quinolinyl]amino]benzoyl]piperazine of melting point 280°-282° C.

1. additionAfter complete addition
2. filtrationThis suspension is then filtered
3. washthe white residue is washed with methylene chloride
4. customdried
5. customThis is re-crystallized from methanol/methylene chloride