| 摘要 |
<p>Cmpds. (I) R' and R2 = Hal A = H or Me Antibacterials and anti-tuberculars, esp. active vs. E. coli, Salmonella typhymurium, and Shigella sonnei. Vs E. coli, min. inhibitory dose = 10gamma/ml. LD50 (p.o., mouse) = 820 mg./kg. Dose 25-250 mg./kg. From 5-chloro-7-iodo-8-hydroxyquinoline (60 g.) in PhH (600 ml.), 100 ml. PhH was distilled off, cooled, and Cl2CHCOCl (32 g.) added over 2.5-3 hrs. at 30-35 deg. The mixture was stirred 5 hrs., filtered, washed with PhH (3 x 50 ml.), and dried in vac., giving (I) (66.5 g.; 81%), m.p. 140.5-141.5 deg.</p> |
