PROCESS FOR THE PREPARATION OF QUINOLONE COMPOUNDS

New quinolone compds. of formula (I) [n=0-2; R1=lower alkyl; R3 = H, lower alkyl, MeO, MeS, halo or CF3 were prepd. by reacting the corresp. 3-halo-methyl compd. with the CH3S or CH3SO2 anion, then opt. oxidising the resulting thioester to CH3SO. Thus, 7- (trifluoromethyl)-4-quinolinol was hydroxyme...

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Bibliographic Details
Main Author DAVIES, ROY V
Format Patent
LanguageEnglish
Korean
Published 28.05.1986
Edition4
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary:New quinolone compds. of formula (I) [n=0-2; R1=lower alkyl; R3 = H, lower alkyl, MeO, MeS, halo or CF3 were prepd. by reacting the corresp. 3-halo-methyl compd. with the CH3S or CH3SO2 anion, then opt. oxidising the resulting thioester to CH3SO. Thus, 7- (trifluoromethyl)-4-quinolinol was hydroxymethylated with HCHO, methylated to the 1-methylquinolinone with Me2SO4, treated with SOCl2, then MeSNa, and the prod. was oxidized to give the sulfoxide or the sulfone. (I) are useful as antihypertensives which may be administered orally, parenterally or rectally. Suitable dosage is 1 - 50 mg/kg/day.
Bibliography:Application Number: KR19810003592