PROCESS FOR OBTAINING AMPHILOXACINE INTERMEDIARY

PCT No. PCT/HU86/00066 Sec. 371 Date Aug. 7, 1987 Sec. 102(e) Date Aug. 7, 1987 PCT Filed Dec. 9, 1986 PCT Pub. No. WO87/03594 PCT Pub. Date Jun. 18, 1987.The invention relates to new 6-fluoro-7-chloro-1-methylamino-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid/boric acid anhydrides of the general F...

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Hauptverfasser: VASVAR L, HORVATH A, KOVACS G, BALOGH M, PAJOR A, HERMECZ I, KERESZTURI G, MESZAROS Z, RITLI P, SIPOS J
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creator VASVAR L
HORVATH A
KOVACS G
BALOGH M
PAJOR A
HERMECZ I
KERESZTURI G
MESZAROS Z
RITLI P
SIPOS J
description PCT No. PCT/HU86/00066 Sec. 371 Date Aug. 7, 1987 Sec. 102(e) Date Aug. 7, 1987 PCT Filed Dec. 9, 1986 PCT Pub. No. WO87/03594 PCT Pub. Date Jun. 18, 1987.The invention relates to new 6-fluoro-7-chloro-1-methylamino-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid/boric acid anhydrides of the general Formula I (I) (wherein R and R1 stand for halogen; an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or an aromatic acyloxy group comprising 7-11 carbon atoms). The new compounds of the general Formula I are valuable intermediates useful in the preparation of the antibacterial agent 6-fluoro-1-methylamino-7-(4-methyl-piperazino)-4-oxo-1,4-dihydro-quino line-3- carboxylic acid. The new compounds of the general Formula I may be prepared by reacting a compound of the Formula II (II) or a compound of the general Formula III (III) (wherein R2 stands for alkyl comprising 1-4 carbon atoms) with hydrogen fluoro borate of the Formula IV HBF4 /IV/ or a borone trihalide of the general Formula V BX3 /V/ (wherein X stands for fluorine, chlorine or bromine) or a complex thereof formed with an ether or a borone derivative of the general Formula VI (VI) (wherein R3, R4 and R5 stand for alkyl comprising 1-5 carbon atoms and optionally substituted by halogen or aryl comprising 6-10 carbon atoms).
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The new compounds of the general Formula I may be prepared by reacting a compound of the Formula II (II) or a compound of the general Formula III (III) (wherein R2 stands for alkyl comprising 1-4 carbon atoms) with hydrogen fluoro borate of the Formula IV HBF4 /IV/ or a borone trihalide of the general Formula V BX3 /V/ (wherein X stands for fluorine, chlorine or bromine) or a complex thereof formed with an ether or a borone derivative of the general Formula VI (VI) (wherein R3, R4 and R5 stand for alkyl comprising 1-5 carbon atoms and optionally substituted by halogen or aryl comprising 6-10 carbon atoms).</description><edition>4</edition><language>eng</language><subject>ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM ; CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; METALLURGY ; ORGANIC CHEMISTRY</subject><creationdate>1987</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=19871231&amp;DB=EPODOC&amp;CC=YU&amp;NR=210786A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,777,882,25545,76296</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=19871231&amp;DB=EPODOC&amp;CC=YU&amp;NR=210786A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>VASVAR L</creatorcontrib><creatorcontrib>HORVATH A</creatorcontrib><creatorcontrib>KOVACS G</creatorcontrib><creatorcontrib>BALOGH M</creatorcontrib><creatorcontrib>PAJOR A</creatorcontrib><creatorcontrib>HERMECZ I</creatorcontrib><creatorcontrib>KERESZTURI G</creatorcontrib><creatorcontrib>MESZAROS Z</creatorcontrib><creatorcontrib>RITLI P</creatorcontrib><creatorcontrib>SIPOS J</creatorcontrib><title>PROCESS FOR OBTAINING AMPHILOXACINE INTERMEDIARY</title><description>PCT No. PCT/HU86/00066 Sec. 371 Date Aug. 7, 1987 Sec. 102(e) Date Aug. 7, 1987 PCT Filed Dec. 9, 1986 PCT Pub. 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No. WO87/03594 PCT Pub. Date Jun. 18, 1987.The invention relates to new 6-fluoro-7-chloro-1-methylamino-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid/boric acid anhydrides of the general Formula I (I) (wherein R and R1 stand for halogen; an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or an aromatic acyloxy group comprising 7-11 carbon atoms). The new compounds of the general Formula I are valuable intermediates useful in the preparation of the antibacterial agent 6-fluoro-1-methylamino-7-(4-methyl-piperazino)-4-oxo-1,4-dihydro-quino line-3- carboxylic acid. The new compounds of the general Formula I may be prepared by reacting a compound of the Formula II (II) or a compound of the general Formula III (III) (wherein R2 stands for alkyl comprising 1-4 carbon atoms) with hydrogen fluoro borate of the Formula IV HBF4 /IV/ or a borone trihalide of the general Formula V BX3 /V/ (wherein X stands for fluorine, chlorine or bromine) or a complex thereof formed with an ether or a borone derivative of the general Formula VI (VI) (wherein R3, R4 and R5 stand for alkyl comprising 1-5 carbon atoms and optionally substituted by halogen or aryl comprising 6-10 carbon atoms).</abstract><edition>4</edition><oa>free_for_read</oa></addata></record>
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subjects ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title PROCESS FOR OBTAINING AMPHILOXACINE INTERMEDIARY
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