Practical synthess of DQ-113,A new quinolone Antibacterial agent,by using the intramolecular Horner-wadsorth-emmons reaction

摘要

A practicla route was developed for synthesizing the C-7 substituten of DQ-113 (6,5-amino-7-[(3S,4R)-4-(1-aminocycloprop-1-yl)-3-fluoro-8-metyl-4-oxoquinolin-3-carboxylic acid),a new quinolone antibacterial agent for serious infectiosn caused by Gram-positive apthogens.The key step was the intramolecular Horner-Wadsworth-Emmons reaction.,In addition,the yield of the final aromatic nucleophilic substitution reaction was improved.