| 摘要 |
<p>PROBLEM TO BE SOLVED: To obtain a quinolone compound or naphthylidone compound, being an effective inhibitors against Helicobacter pylori infectious diseases, thus useful for preventing/treating digestive ulcer and gastritis, etc. SOLUTION: This new compound (or pharmaceutically permissible salt thereof) is shown by formula I [R<1> is H or a (substituted) phenyl, etc.; R<2> is a 1-10C alkyl, furyl, etc.; R<3> is a 1-4C alkyl, phenyl, etc.; R<4> to R<7> are each H, a 1-3C alkyl, etc. ; X, Y and Z are each C or N], e.g. 4-oxo-4H-quinoline-1,3- dicarboxylic acid 1-t-butyl ester 3ethyl ester. The compound of formula I is obtained by the following process: a compound of formula II is reacted with di-t-butyl dicarbonate in the presence of a base followed by introducing R<2> group into the reaction product under Grignard reaction conditions to form into a compound of formula III, which, in turn, is reacted with a compound of the formula R<3> L (L is an eliminable group) in the presence of a base, and the resultant compound is freed from two carboxylic ester groups to obtain a compound of formula IV, which, in turn, is dehydrogenated with DDQ (2,3- dichloro-5, 6dicyano-1,4-benzoquinone).</p> |
