反应详情

A mixture of N-[(4-Chlorophenyl)methyl]-8-fluoro-4-hydroxy-6-[3-(methylthio)-1-propynyl]-3-quinolinecarboxamide from Example No. 126 (0.07 g) and Pd/C (10%, 0.120 g) in 3:1 CH2Cl2 /MeOH (20 mL) was placed on a Parr hydrogenator under 45 psi of H2 and shaken for 4 h. Another 0.08 g of Pd/C was added, and the resulting mixture is shaken for 2 h. The reaction mixture is then filtered through Celite, 0.120 g of fresh catalyst was added, and the resulting mixture was shaken under H2 for 6 h. The reaction mixture is then filtered through Celite and concentrated in vacuo. Crystallization from EtOH gave 0.015 g of the title compound as a solid.

1. stirringthe resulting mixture is shaken for 2 h
2. filtrationThe reaction mixture is then filtered through Celite, 0.120 g of fresh catalyst
3. additionwas added
4. stirringthe resulting mixture was shaken under H2 for 6 h
5. filtrationThe reaction mixture is then filtered through Celite
6. concentrationconcentrated in vacuo
7. customCrystallization from EtOH