Processing

Please wait...

Settings

Settings

1. WO2000040549 - METHOD FOR PRODUCING ROBENIDINE OR DERIVATIVES THEREOF

Publication Number WO/2000/040549
Publication Date 13.07.2000
International Application No. PCT/EP2000/000050
International Filing Date 05.01.2000
Chapter 2 Demand Filed 30.06.2000
IPC
C07C 277/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
277Preparation of guanidine or its derivatives, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups
08of substituted guanidines
C07C 281/18 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
281Derivatives of carbonic acid containing functional groups covered by groups C07C269/-C07C279/128
16Compounds containing any of the groups e.g. aminoguanidine
18the other nitrogen atom being further doubly-bound to a carbon atom, e.g. guanylhydrazones
CPC
C07C 277/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
277Preparation of guanidine or its derivatives, i.e. compounds containing the group , the singly-bound nitrogen atoms not being part of nitro or nitroso groups
08of substituted guanidines
C07C 281/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
281Derivatives of carbonic acid containing functional groups covered by groups C07C269/00 - C07C279/00 in which at least one nitrogen atom of these functional groups is further bound to another nitrogen atom not being part of a nitro or nitroso group
16Compounds containing any of the groups , e.g. aminoguanidine
18the other nitrogen atom being further doubly-bound to a carbon atom, e.g. guanylhydrazones
Applicants
  • LONZA AG [CH/CH]; Münchensteinerstrasse 38 CH-4052 Basel, CH (AllExceptUS)
  • HANSELMANN, Paul [CH/CH]; CH (UsOnly)
  • HILDEBRAND, Stefan [CH/CH]; CH (UsOnly)
Inventors
  • HANSELMANN, Paul; CH
  • HILDEBRAND, Stefan; CH
Agents
  • RITTHALER, Wolfgang ; Winter, Brandl et al. Alois-Steinecker-Strasse 22 D-85354 Freising, DE
Priority Data
60/146,10729.07.1999US
99100097.706.01.1999EP
Publication Language German (DE)
Filing Language German (DE)
Designated States
Title
(DE) VERFAHREN ZUR HERSTELLUNG VON ROBENIDIN BZW. DESSEN DERIVATE
(EN) METHOD FOR PRODUCING ROBENIDINE OR DERIVATIVES THEREOF
(FR) PROCEDE DE PRODUCTION DE ROBENIDINE ET DE SES DERIVES
Abstract
(DE)
Beschrieben wird ein neues Verfahren zur Herstellung von Robenidin bzw. dessen Derivate der allgemeinen Formel (I), worin X ein Halogenatom bedeutet, ausgehend von Hydrazinhydrat und einer Cyanverbindung. Dabei werden die beiden Edukte zunächst in einem C1-4-Alkohol, einem C1-4-Alkohol-Wasser-Gemisch als Lösungsmittel oder in einem aprotischen polaren organischen Lösungsmittel in ein Diaminoguanidin der allgemeinen Formel (III) überführt, worin Y ein Halogenatom oder Tosyl bedeutet, welches dann direkt ohne Isolation mit einem p-Halogenbenzaldehyd der allgemeinen Formel (IV) in einem C1-4-Alkohol, einem C1-4-Alkohol-Wasser-Gemisch oder in einem aprotischen polaren organischen Lösungsmittel-Wasser-Gemisch als Lösungsmittel zum Endprodukt umgesetzt wird.
(EN)
The invention relates to a novel method for producing robenidine or derivatives thereof of general formula (I) wherein X means a halogen atom, using hydrazine hydrate and a cyanogen compound as the starting materials. The two educts are first converted into a diaminoguanidine of general formula (III) in a C1-4 alcohol or a C1-4 alcohol-water mixture as the solvent or in an aprotic polar organic solvent, Y being a halogen atom or tosyl. Said diaminoguanidine is then directly reacted with a p-halobenzaldehyde of general formula (IV) without isolation in a C1-4 alcohol, a C1-4 alcohol-water mixture or in an aprotic polar organic solvent-water mixture as the solvent to form the end product.
(FR)
L'invention concerne un nouveau procédé de production de robénidine et de ses dérivés de la formule générale (I), où X représente un atome d'halogène, à partir d'hydrate d'hydrazine et d'une liaison de cyan. Tout d'abord, dans un alcool C1-4 ou dans un mélange eau-alcool C1-4 Utilisé comme solvant ou dans un solvant organique polaire aprotique, les deux matières premières d'alimentation se transforment en guanidine diammonique de la formule générale (III) où Y représente un atome d'halogène ou du tosyl. Ensuite dans un alcool C1-4, dans un mélange eau-alcool C1-4 ou dans un mélange eau-solvant organique polaire aprotique utilisé comme solvant, la guanidine diammonique réagit avec un p-halogènbenzaldehyde de la formule générale (IV), directement sans isolement, pour donner un produit final.
Also published as
US09899738
US09900409
Latest bibliographic data on file with the International Bureau