| 摘要 |
<p>6-Fluoro 1,4-dihydro 4-oxo 7-piperazinyl quinoline 3-carboxylic acid derivs. of formula (I), in which R1 and R2 can be various radicals, and their suitable addn. salts and hydrates, are made by (a) reaction of a cpd. of formula (II) with diethanolamine opt. substd. with R1, R3 being H or lower alkyl and X being Cl or Br; (b) conversion to the acid chloride; (c) reaction with a dialkyl malonate; (d) decarboxylation by heating in water in presence of p-toluene sulphonic acid; (e) reaction with ethyl o-formate and an amine of formula R2NH2; (f) heating in organic solvent in presence of an acid acceptor; and (g) soln. in aq. alkali.</p> |
