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1. WO1997024335 - PROCESS FOR THE PREPARATION OF 3-DIHALOBENZYL-2,4-QUINAZOLINEDIONE DERIVATIVES

Publication Number WO/1997/024335
Publication Date 10.07.1997
International Application No. PCT/JP1996/003878
International Filing Date 27.12.1996
Chapter 2 Demand Filed 09.06.1997
IPC
C07C 227/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
227Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
04Formation of amino groups in compounds containing carboxyl groups
06by addition or substitution reactions, without increasing the number of carbon atoms in the carbon skeleton of the acid
08by reaction of ammonia or amines with acids containing functional groups
C07C 229/56 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
52having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
54with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring
56with amino and carboxyl groups bound in ortho- position
C07D 239/96 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
72Quinazolines; Hydrogenated quinazolines
95with hetero atoms directly attached in positions 2 and 4
96Two oxygen atoms
CPC
C07C 227/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
227Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
04Formation of amino groups in compounds containing carboxyl groups
06by addition or substitution reactions, without increasing the number of carbon atoms in the carbon skeleton of the acid
08by reaction of ammonia or amines with acids containing functional groups
C07D 239/96
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
72Quinazolines; Hydrogenated quinazolines
95with hetero atoms directly attached in positions 2 and 4
96Two oxygen atoms
Applicants
  • FUJI CHEMICAL INDUSTRY CO., LTD. [JP]/[JP] (AllExceptUS)
  • FUJISAWA PHARMACEUTICAL CO., LTD. [JP]/[JP] (AllExceptUS)
  • KAMIYA, Takashi [JP]/[JP] (UsOnly)
  • TAKEHARA, Hiroyuki [JP]/[JP] (UsOnly)
  • INAMOTO, Yoshitaka [JP]/[JP] (UsOnly)
  • TANIGUCHI, Akihito [JP]/[JP] (UsOnly)
  • MASUMOTO, Masayuki [JP]/[JP] (UsOnly)
Inventors
  • KAMIYA, Takashi
  • TAKEHARA, Hiroyuki
  • INAMOTO, Yoshitaka
  • TANIGUCHI, Akihito
  • MASUMOTO, Masayuki
Agents
  • KOTANI, Etsuji
Priority Data
7/34374728.12.1995JP
7/34374828.12.1995JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) PROCESS FOR THE PREPARATION OF 3-DIHALOBENZYL-2,4-QUINAZOLINEDIONE DERIVATIVES
(FR) PROCEDE DE FABRICATION DES DERIVES DE LA 3-DIHALOBENZYL-2,4-QUINAZOLINEDIONE
Abstract
(EN)
A process for preparing 3-dihalobenzyl-2,4-quinazolinedione derivatives of general formula (V) (wherein X1, X2, and X3 are each halogeno; and A is alkylene) by reacting a dihalobenzyl derivative of general formula (III) (wherein L is an acid residue; and X2 and X3 are each as defined above) with a carboxylalkylated 2,4-quinazolinedione derivative of general formula (I) (wherein X1 and A are each as defined above) to selectively replace the imino hydrogen atom of the derivative (I). The above process enables the efficient preparation of the compounds of general formula (V) useful as inhibitors against aldose reductases, makes it possible to secure the safety and hygiene of workers, and can facilitate waste disposal to reduce the expenses, thus being industrially extremely advantageous.
(FR)
Procédé de préparation des dérivés de la 3-dihalobenzyl-2,4-quinazolinedione, de formule générale (V), où X1, X2 et X3 sont halogéno et A est alkylène, dans lequel on fait réagir un dérivé dihalobenzyle de formule générale (III), où L est un reste acide, et X2 et X3 sont tels que définis ci-dessus, avec un dérivé de la 2,4-quinazolinedione carboxylalkylée de formule générale (I), où X1 et A sont tels que définis ci-dessus, pour remplacer sélectivement l'atome imino-hydrogène du dérivé (I). Du fait que le procédé ci-dessus permet de préparer avec un bon rendement les composés de formule générale (V) utiles comme inhibiteurs des aldose-réductases, d'assurer la sécurité et l'hygiène des travailleurs et de faciliter le rejet des déchets pour réduire les coûts, il est très intéressant du point de vue industriel.
Also published as
Latest bibliographic data on file with the International Bureau