FARMACEUTSKO-HEMIJSKA INDUSTRIJA "ZDRAVLJE"a.d.CENTAR ZA ISTRAŽIVANJE I RAZVOJ
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Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems
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Abstract
Razvijen je jednostavan i za primenu pogodan postupak dobijanja antibiotika iz grupe fluorohinolonskih derivata, opšte formule (I) gde R i R2 označavaju atom vodonika, ili alkil grupu sa C1-C4, a R1 označava alkil grupu sa C1-C4 ili cikloalkil grupu (kao na primer ciklopropil grupu), i/ili njihovih soli ili hidrata, reakcijom piperazina ili derivata plperazina sa jedinjenjem opšte formule VI u inertnom rastvaraču farmakopejske čistoće, na povećanoj temperaturi. Niža temperatura reakcije, rad na atmosferskom pritisku, tehnička jednostavnost postupka prečišćavanja prevodjenjem i izolovanjem u obliku farmaceutski prihvatljivih soli, povećanje prlnosa, pojeftinjenje postupka za industrijsku primenu, kao i farmakopejska čistoća proizvoda omogućuju njihiovu primenu kao antibiotika u humanoj i veterinarskoj medicini.A simple and convenient application for the preparation of antibiotics from the group of fluoroquinolone derivatives of the general formula (I) is developed wherein R and R2 denote a hydrogen atom or an alkyl group with C1-C4 and R1 denotes an alkyl group with a C1-C4 or cycloalkyl group (as for example cyclopropyl group), and / or their salts or hydrates, by reaction of piperazine or a plperazine derivative with a compound of general formula VI in an inert pharmacopoeial purity solvent at elevated temperature. The lower reaction temperature, atmospheric pressure operation, the technical simplicity of the translation and isolation purification process in the form of pharmaceutically acceptable salts, the increase in dirt, the cheapening of the process for industrial application, as well as the pharmacopoeial purity of the products allow their use as antibiotics in human and veterinary medicine.
YU53401A2001-07-252001-07-25A process for synthesis of fluoroquinolonic derivatives
YU53401A
(en)
PROCEDURE TO PREPARE DERIVATIVES OF 9-DESOXO-9A-AZA-9A-HOMOERITROMICINA A 4 '' - REPLACED, INTERMEDIARY AND PROCEDURE FOR THE PREPARATION OF THE SAME
1 ,4-BENZOTHIAZEPINE-l, l-DIOXIDE DERIVATIVES SUBSTITUTED BY SUGAR RADICALS, METHOD FOR THE PRODUCTION THEREOF, MEDICAMENTS CONTAINING THESE COMPOUNDS AND THE USE THEREOF