| 摘要 |
<p>PURPOSE: To obtain a new quinolinecarboxylic derivative, having high antimicrobial action, reduced in adverse effects such as phototoxicity, induction, etc., of a chromosomal aberration and a spasm and useful as an antimicrobial agent. CONSTITUTION: This compound of formula I (asymmetric carbon marked with *is the S-configuration; R<1> is methyl or ethyl) and its pharmacologically permissible salt, e.g. 5-amino-7-((3S,4S)-3amino-4-methyl-1-pyrrolidinyl)-1-cyclopropyl-6- fluoro-1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acid, is obtained by reacting, e.g. a 7-halogenoquinoline-3-carboxylic acid derivative of formula II (R<5> is H or a lower alkyl; X is a halogen, preferably F or Cl, especially preferably F) with a pyrrolidine derivative of formula III (R<3> and R<4> are each independently H or an amino-protecting group), providing a compound of formula IV (R<2> is H, BF2 , etc.) which is a synthetic intermediate and, at need, carrying out the deprotection of R<3> and R<4> and hydrolysis of the ester of R<2> .</p> |
