| 摘要 |
<p>Derivs. of 2-methyl-5-nitro-8-hydroxyquinoline of formula (I) and therapeutic compns. contng. them. R = aliphatic, heterocyclic or aromatic radical Z = aromatic or heterocyclic radical, opt. substd. by NO2. As bacteriostatic, bactericidal, fungicidal, amoebicidal, trichomonacidal and anthelmintic agents. (a) A mixt. of 2-methyl-5-nitro-8-hydroxyquinoline (204 g.), 5-nitro-2-furaldehyde (145 g.), Ac2O (435 g.) and anhyd. NaOAc (24 g.) is refluxed for 3 hrs. to give 1-(5'-nitro-8'-acetoxyquinolinyl-2')-2-(5'-nitro-alpha-furyl)ethy- lene (69%), m.p.211:2 deg. (MeCOEt), hydrolysis of which gives the 8-OH cpd., m.p.305-6 deg. (b) this (32.7 g.) and pyridine (700 ml) at 5 deg. are treated with furoyl chloride (14.3 g.) and the mixt. stirred for 12 hrs. to give 1-(5'-nitro-8'-furoyloxyquinolinyl-2')-2-(5'-nitro-alpha-furyl)et- hylene (74%), m.p.246-8 deg. (dioxan).</p> |
