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1. EP0185679 - INTERMEDIARY PRODUCTS OF CEPHALOSPORINE, PREPARATION PROCESS THEREOF AND UTILIZATION THEREOF

Office European Patent Office
Application Number 85902014
Application Date 04.04.1985
Publication Number 0185679
Publication Date 02.07.1986
Publication Kind B1
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
277
Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02
not condensed with other rings
20
having two or three double bonds between ring members or between ring members and non-ring members
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
501
Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula: , e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
02
Preparation
04
from compounds already containing the ring or condensed ring systems, e.g. by dehydrogenation of the ring, by introduction, elimination or modification of substituents
06
Acylation of 7-aminocephalosporanic acid
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
277
Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02
not condensed with other rings
20
having two or three double bonds between ring members or between ring members and non-ring members
32
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38
Nitrogen atoms
40
Unsubstituted amino or imino radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
277
Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
60
condensed with carbocyclic rings or ring systems
62
Benzothiazoles
68
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
70
Sulfur atoms
74
Sulfur atoms substituted by carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
501
Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula: , e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
02
Preparation
04
from compounds already containing the ring or condensed ring systems, e.g. by dehydrogenation of the ring, by introduction, elimination or modification of substituents
06
Acylation of 7-aminocephalosporanic acid
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
501
Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula: , e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
14
Compounds having a nitrogen atom directly attached in position 7
16
with a double bond between positions 2 and 3
20
7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
24
with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
38
Methylene radicals, substituted by nitrogen atoms; Lactams thereof with the 2-carboxyl group; Methylene radicals substituted by nitrogen-containing hetero rings attached by the ring nitrogen atom; Quaternary compounds thereof
46
with the 7-amino radical acylated by carboxylic acids containing hetero rings
C 07D
C07D 277/20
C 07D
C07D 277/40
C07D 277/74
C07D 417/12
CPC
C07D 277/587
C07D 417/12
Applicants BIOCHEMIE GESELLSCHAFT M.B.H.
Inventors ASCHER, GERD
STURM, HERBERT
THALER, HEINRICH
VEITH, WERNER
Priority Data 119784 10.04.1984 AT
119884 10.04.1984 AT
Title
(DE) CEPHALOSPORINZWISCHENPRODUKTE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG.
(EN) INTERMEDIARY PRODUCTS OF CEPHALOSPORINE, PREPARATION PROCESS THEREOF AND UTILIZATION THEREOF
(FR) PRODUITS INTERMEDIAIRES DE CEPHALOSPORINE, LEUR PROCEDE DE PREPARATION ET LEUR UTILISATION.
Abstract
(EN)
Process for preparing intermediary products of cephalosporine having the formula (I) wherein R1 is an acyl group. Modification of a compound having the formula (IV) and/or (IVa) wherein R1 has the same meaning as hereabove and (A), respectively (B) represents a heterocycle having 5 or 6 atoms, and comprising in addition to the N atom one or two other heteroatoms, for example O, N and S, and susceptible of being substituted or ringed with an optionally substituted benzol cycle, with a compound of formula (V) wherein R10 represents hydrogen or an amino protection group.

(FR)
Procédé de préparation de produits intermédiaires de céphalosporine de formule (I) où R1-CO représente un groupe acyle. Modification d'un composé de formule (IV) et/ou (IVa) où R1 a la même signification que ci-dessus et (A), respectivement (B) représente un hétérocycle comportant 5 ou 6 atomes, pouvant comporter en plus de l'atome de N un ou deux autres hétéroatomes, par exemple O, N et S, et pouvant être substitué ou annelé avec un cycle benzol le cas échéant substitué, avec un composé de formule (V) où R10 représente un hydrogène ou un groupe de protection amino.