Substd quinoline carboxylic acid prepn useful for antibiotic prodn - by reacting acetophenone with alkane carboxylic acid chloride or anhydride, then with tri:methyl ortho:formate and amine, cyclising and oxidn

摘要

Substd. quinoline carboxylic acids of formula (I) in which R is a salient gp.; R1 is an aliphatic or aromatic gp.; and R4 is F, H or acetoxy, are made by (a) reacting an acetophenone with an alkane carboxylic acid chloride or anhydride in a soln. of a boron cpd. in the alkane carboxylic acid to give (II); (b) reacting with acetic anhydride and trimethyl orthoformate and treating the prod. with an amine R1NH2; (c) cyclising in presence of Pt, Ni or Pd salts as catalyst and a base to give (III); and (d) oxidising to form cpd. of formula (I).