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Title:
INTERMEDIATE IN MANUFACTURE OF ANTIBACTERIAL AGENT
Document Type and Number:
Japanese Patent JPH0748354
Kind Code:
A
Abstract:

PURPOSE: To provide a novel intermediate composed of a 5-amino-1- cycloalkyl-1,4-dihydro-4-oxo-6-fluoroquinoline-3-carboxylic acid derivative and useful as the starting material for preparing antibacterial agents.

CONSTITUTION: To a THF solution of a malonic acid half ester is added 2,2'- bipyridine and the reaction is carried out by adding n-butyllithium and 2- nitro-3,4,5,6-tetrafluorobenzoyl chloride thereto to form ethyl 2-nitro-3,4,5,6- tetrafluoro-β-oxobenzenepropanoate which is then reacted with triethyl orthoformate and acetic anhydride to obtain ethyl 1-cyclopropyl-5-nitro-6,7,8- trifluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylate. Then, by reducing this compound is obtained a desired intermediate compound (salt) having the formula (wherein L is F or Cl; X is CH, CF or N; R1 is H, 1-6C al-kyl or the like; and R2 is 3-6C cycloalkyl) in manufacturing antibacterial agents.


Inventors:
TOMASU EFU MITSUKU
JIYOZEFU PII SANSHIEZU
JIYON EMU DOOMAGARA
Application Number:
JP17242094A
Publication Date:
February 21, 1995
Filing Date:
July 25, 1994
Export Citation:
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Assignee:
WARNER LAMBERT CO
International Classes:
C07D215/56; A61K31/435; A61K31/47; A61P31/04; C07D401/04; C07D471/04; C07D471/10; C07D487/10; C07D498/06; C07D513/00; C07D519/00; (IPC1-7): C07D215/56
Domestic Patent References:
JPS58174367A1983-10-13
JPS5777683A1982-05-15
JPS5874667A1983-05-06
Attorney, Agent or Firm:
Chika Takagi (2 outside)



 
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