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1. CN1235605 - Preparation of naphthyridine compounds and intermediate products

Amt China
Aktenzeichen/Anmeldenummer 97199280.0
Anmeldedatum 17.10.1997
Veröffentlichungsnummer 1235605
Veröffentlichungsdatum 17.11.1999
Veröffentlichungsart A
IPC
C07D 213/26
CSektion C Chemie; Hüttenwesen
07Organische Chemie
DHeterocyclische Verbindungen
213Heterocyclische Verbindungen, die sechsgliedrige Ringe mit 1 Stickstoffatom als einziges Ring- Heteroatom enthalten, die nicht mit anderen Ringen kondensiert sind und die drei oder mehr Doppelbindungen innerhalb des Rings oder zwischen Ringatomen und Atomen außerhalb des Rings enthalten
02mit drei Doppelbindungen innerhalb des Rings oder zwischen Ringatomen und Atomen außerhalb des Rings
04wobei keine Bindung zwischen Ring- Stickstoffatom und einem Nichtringglied besteht, oder nur Wasserstoffatome oder Kohlenstoffatome direkt an das Ring- Stickstoffatom gebunden sind
24mit an Ring-Kohlenstoffatome gebundenen substituierten Kohlenwasserstoffresten
26durch Halogenatome oder Nitrogruppen substituierte Reste
C07D 471/04
CSektion C Chemie; Hüttenwesen
07Organische Chemie
DHeterocyclische Verbindungen
471Heterocyclische Verbindungen, die im kondensierten System Stickstoffatome als einzige Ring-Heteroatome enthalten, wobei mindestens ein Ring ein sechsgliedriger Ring mit einem Stickstoffatom ist, soweit nicht in den Gruppen C07D451/-C07D463/274
02in welchen das kondensierte System zwei Heteroringe enthält
04ortho-kondensierte Systeme
//(C07D471/04,221:00,221:00)
CPC
C07D 211/84
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
80having two double bonds between ring members or between ring members and non-ring members
84with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms
C07D 213/26
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
24with substituted hydrocarbon radicals attached to ring carbon atoms
26Radicals substituted by halogen atoms or nitro radicals
C07D 213/61
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
61Halogen atoms or nitro radicals
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Anmelder Bayer AG
拜尔公司
Erfinder S. Antons
S·安东斯
R. Gehring
R·格林
T. Beitzke
T·比尔菲尔德特
B·贝茨克
Vertreter wang jingchao
中国专利代理(香港)有限公司
中国专利代理(香港)有限公司
Titel
(EN) Preparation of naphthyridine compounds and intermediate products
(ZH) 制备萘啶化合物的方法以及新的中间体
Zusammenfassung
(EN)
Disclosed is a method of producing naphthyridine compounds of formulae (Ia) to (1c) wherein R means hydrogen or C1-C4 alkyl, Ar means possibly substituted phenyl, Hal means independently fluorine, chlorine or bromine, and n stands for 1, 2 or 3, whereby a halogenated nicotinic, isonicotinic or picolinic acid is made to react with an amino acrylic acid ester to obtain a halogenated 2-nicotinoyl-, isonicotinoyl- or picolinoyl-3-aminoacrylate which is made to react with an optionally substituted aniline to obtain a halogenated 2-nicotinoyl-, isonicotinoyl- or picolinoyl-3-aminoacrylate which contains an amino group corresponding to the optionally substituted aniline. The second halogenated 2-nicotinoyl-, isonicotinoyl- or picolinoyl-3-aminoacrylate is cyclized by adding an acid scavenger to a compound of formulae (Ia) to (Ic) with R = C1-C4 alkyl and, in the case of production of a compound of formulae (Ia) to (Ic) with R = H, the compound of the formulae (Ia) to (Ic) with R = C1-C4 alkyl is saponified.

(ZH)

公开了一种生产式(Ⅰa)-(Ⅰc)萘啶化合物的方法,其中R是氢或C1-C4-烷基,Ar是任选被取代的苯基,Hal彼此独立地是氟、氯或溴,n是1、2或3,该方法包括,将卤代的烟酸、异烟酸或吡啶甲酸与氨基丙烯酸酯反应生成卤代的2-烟酰基-、异烟酰基-或吡啶甲酰基-3-氨基丙烯酸酯,将其与任选被取代的苯胺反应生成卤代2-烟酰基-、异烟酰基-或吡啶甲酰基-3-氨基丙烯酸酯,其中含有相应于任选被取代的苯胺的氨基。将后一种卤代的2-烟酰基-、异烟酸基-或吡啶甲酰基-3-氨基丙烯酸酯通过加入酸清除剂进行环化生成其中R=C1-C4-烷基的式(Ⅰa)-(Ⅰc)化合物,当要制备其中R=H的式(Ⅰa)-(Ⅰc)的化合物时。将其中R=C1-C4-烷基的式(Ⅰa)-(Ⅰc)化合物皂化。