DEUTSCHES PATENT- UND MARKENAMT
Class/Subcl.:
German Patent and Trade Mark Office
C07D
Date : January 14th, 2005
DE - Proposal — TE 107
Rapporteur Proposal for project TE 107 (existing example No. A 11)
Level/Category (ies)
CL
AL
1a, 1b, 2a, 2d, 3
1a, 1b, 2a, 2d, 3
Documents (Classification is based on underlined document)
GB 1 278 757
DE 2 107 405 A
FR 2 079 880
JP 49080066 A
Short Version of the Disclosure
The document discloses a method for the preparation of 5-nitroimidazole derivatives of the
general formula
N
O2N
R2
N
OH
R1
wherein R1 is a straight- or branched-chain alkyl group containing 1 to 6 carbon atoms and
R2 is a straight- or branched-chain alkyl group containing 1 to 4 carbon atoms which
comprises the nitration of an imidazole derivative of the general formula
N
R2
N
OR3
R1
wherein R1 and R2 are as above defined, and R3 is a radical which protects the hydroxyl
group during the nitration reaction and is easily removable by hydrolysis. The nitration of the
imidazoles, and hydrolysis of the 5-nitroimidazole compound liberating the hydroxyl group is
carried out by any known method (see claim 1).
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5-nitroimidazole derivatives possess chemotherapeutic properties; they are active as antiprotozoal, amoebicides and trichomonacides.
Representative Prior Art
GB 1079271 - Processes for the preparation of 5-nitroimidazole derivatives involving the
reaction of a reactive ester reactant resp. an epoxide with a derivative of nitroimidazol.
Invention Information
I1: Process for the preparation of 5-nitroimidazole derivatives which comprises the nitration
of an imidazole derivative, and hydrolysis of the resulting 5-nitroimidazole compound (see
claims 1 to 8).
I2: Process for the preparation of 5-nitroimidazole derivatives as described in the foregoing
example (see claim 9).
I3: 5-Nitroimidazole derivatives of the general formula specified in claim 1 when prepared by
the process claimed in any one of I1 or I2 (see claim 18).
Additional Information
5-Nitroimidazole derivatives obtained by the process described possess chemotherapeutic
properties (see description page 1, lines 9 to 21).
Identification of Potential Subclasses
Subject Matter
Tool
Query
IPC Places
I1
Catchword Index
General processes for the preparation
of HETEROCYCLIC
C07D
I2
Catchword Index
General processes for the preparation
of HETEROCYCLIC
I3
Catchword Index
A1
Note 4 under title
C07D
COMPOUNDS
COMPOUNDS
HETEROCYCLIC
COMPOUNDS
THERAPEUTIC ACTIVITY
C07D
C07D
A61P
Analysis and Selection of Classification Symbols
Core Level
Processes for the preparation of derivatives of 5-Nitroimidazole, a heterocyclic compound,
are of interest. As according to Note 3 under C07 class notes chemical compounds as well
as their preparations are classified in the groups for the type of compound prepared,
using the catchword “heterocyclic compounds” leads to subclass C07D. Following the
Subclass Index, compounds containing one hetero ring, having Nitrogen as a ring hetero
atom, having two nitrogen atoms in a five-membered ring, whereas the heterocyclic
compounds contain 1,3-diazole rings and are not condensed with other rings, are classified
in the main group 233/00.
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5-Nitroimidazole possesses chemotherapeutic properties and is therefore classified in A61P.
Antiparasitic agents are covered by A61P33/00, therefore this group is an appropriate place.
Advanced Level
Following the arguments under “Core level” the advanced level is more finely subdivided in
C07D233/00. Regarding the last appropriate place according to Note 5(a) under the subclass
title, C07D233/94 applies here as there are two double bonds between ring members with
nitro radicals attached in position 4 or 5 and hydrocarbon radicals, substituted by oxygen,
attached to other ring members.
Subject Matter
Anaylsis of
Subclass
Selection
Subcalss
Analysis of
Group
Selection
IPC CL
IPC (2006)
IPC AL
I1
Rule 5(a) under
sublcass title
Rule 5(a) under
sublcass title
Rule 5(a) under
sublcass title
Note 4 under
subclass title C07D
C07D
Last place rule
C07D233/00
C07D233/94
C07D
Last place rule
C07D233/00
C07D233/94
C07D
Last place rule
C07D233/00
C07D233/94
A61P
Common rule
A61P33/00
A61P33/02
A61P33/04
I2
I3
A1
Complete Classification
The complete core and advanced level classification for this document based on the above
analysis is as follows:
Core Level
Int.Cl.(2006)
C07D233/00
A61P 33/00
Advanced Level
C07D 233/94 (2006.01)
A61P 33/02 (2006.01)
A61P 33/04 (2006.01)
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