CH311678A - Process for the production of a new basic substituted fatty acid amide. - Google Patents

Process for the production of a new basic substituted fatty acid amide.

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Publication number
CH311678A
CH311678A CH311678DA CH311678A CH 311678 A CH311678 A CH 311678A CH 311678D A CH311678D A CH 311678DA CH 311678 A CH311678 A CH 311678A
Authority
CH
Switzerland
Prior art keywords
diethylamine
ethyl
methyl
fatty acid
methoxyphenoxy
Prior art date
Application number
Other languages
German (de)
Inventor
Aktiengesellschaft Cilag
Original Assignee
Cilag Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Cilag Ag filed Critical Cilag Ag
Publication of CH311678A publication Critical patent/CH311678A/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/02Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Description

  

  



  Verfahren zur Herstellung eines neuen basisch substituierten   Fettsäureamides.   



   Gegenstand des vorliegenden Patentes bil  clet    ein Verfahren zur Herstellung eines neuen basiseh substituierten   Fettsäureamides,    welches   dadureh gekennzeichnet    ist, dass man eine Verbindung der Formel
EMI1.1     
 in welcher X einen reaktionsfähigen, während der Reaktion sich abspaltenden Rest bedeutet, mit Diäthylamin umsetzt.



   Der Rest X kann in einem Halogenatom oder einem sonstigen für den Austausch gegen den basischen Rest geeigneten reaktionsfähigen Substituenten, wie z.   B.    einer Alkylsulfonyloxy-oder Arylsulfonyloxygruppe, beste  hen.    Der Austausch der Gruppe X gegen den Diäthylaminrest erfolgt z. B. durch einfaches Erwärmen mit Diäthylamin, gegebenenfalls in Gegenwart eines basisch reagierenden Kondensationsmittels, oder von Diäthylamin im   Überschuss.    Das   N- [2- (3'-Methoxy-phenoxy)-    äthyl-1]-N-methyl-diäthylaminoaeetamid ist ein farbloses, unter 0,06 mm bei   157-158     siedendes   01.   



   Das neue Amid soll als   Lokalanästhetikum    und als Zwischenprodukt zur Herstellung weiterer Derivate Verwendung finden.



   Beispiel :
25,8 g N- [2-   (3'-Methoxy-phenoxy)-äthyl-1]-    N-methyl-ehloraeeta, mid und 22 g Diäthylamin werden zusammen in   150      mS    abs. Benzol 6 Stunden auf dem Wasserbad erhitzt. Das Re  aktionsgemisch    h wird mit Wasser   ausgeschüt-    telt und dann mit 2n-Salzsäure ausgezogen.



  Darauf wird der salzsaure Auszug mit Äther extrahiert, unter Eiskühlung mit konz. Natronlauge versetzt und das ausgesehiedene öl in Äther aufgenommen. Nach dem Trocknen   der Ätherauszüge über Pottasche wird    der Äther verdampft und der Rüekstand im Hochvakuum destilliert.



   Dabei gewinnt man das unter 0,06 min bei 157-158  siedende N- [2- (3'-Methoxy-phen  oxy)-äthyl-1]-N-methyl-diäthylaminoacetamid    als farbloses,   säurelösliches 01.     



   PATENTANSPRUCH :
Verfahren zur Herstellung eines neuen basisch substituierten   Fettsäureamides,    da  dureh    gekennzeichnet, dass man eine Verbindung der Formel
EMI1.2     
 in welcher X einen reaktionsfähigen,   wahrend    der Reaktion sich abspaltenden Rest bedeutet, mit Diäthylamin umsetzt. Das auf diese Weise erhaltene N- [2- (3'-Methoxy-phenoxy)-äthyl   1]-N. methyl-diäthylaminoacetamid bildet ein    farbloses, unter 0,06 mm bei 157-158  siedendes   01.   



   Das neue Amid soll als   Lokalanästhetikum    und als   Zwisehenprodukt    Verwendung finden.



   UNTERANSPRUCH :
Verfahren nach Patentanspruch, dadurch gekennzeichnet, dass man ein N- [2- (3'-Methoxy   phenoxy)-äthyl-1]-N-methyl-halogen-acetamid    mit Diäthylamin reagieren lässt. 

**WARNUNG** Ende DESC Feld konnte Anfang CLMS uberlappen**.





  



  Process for the production of a new basic substituted fatty acid amide.



   The subject of the present patent bil clet a process for the preparation of a new basic substituted fatty acid amide, which is characterized by the fact that a compound of the formula
EMI1.1
 in which X is a reactive radical which is split off during the reaction, is reacted with diethylamine.



   The radical X can be in a halogen atom or any other reactive substituent suitable for replacement with the basic radical, such as. B. an alkylsulfonyloxy or arylsulfonyloxy group, best hen. The exchange of group X against the diethylamine residue takes place z. B. by simply heating with diethylamine, optionally in the presence of a basic condensing agent, or diethylamine in excess. The N- [2- (3'-methoxyphenoxy) - ethyl-1] -N-methyl-diethylaminoaetamide is a colorless oil that boils below 0.06 mm at 157-158.



   The new amide will be used as a local anesthetic and as an intermediate for the production of other derivatives.



   Example:
25.8 g of N- [2- (3'-methoxyphenoxy) ethyl-1] - N-methyl-ehloraeeta, mid and 22 g of diethylamine are dissolved together in 150 mS abs. Benzene heated on a water bath for 6 hours. The reaction mixture h is extracted by shaking with water and then extracted with 2N hydrochloric acid.



  The hydrochloric acid extract is then extracted with ether, with conc. Sodium hydroxide solution was added and the separated oil was absorbed in ether. After the ether extracts have dried over potash, the ether is evaporated and the residue is distilled in a high vacuum.



   The N- [2- (3'-methoxyphenoxy) -ethyl-1] -N-methyl-diethylaminoacetamide, which boils at 157-158 for less than 0.06 min, is obtained as colorless, acid-soluble oil.



   PATENT CLAIM:
Process for the preparation of a new basic substituted fatty acid amide, characterized by the fact that one is a compound of the formula
EMI1.2
 in which X is a reactive radical which is split off during the reaction, reacts with diethylamine. The N- [2- (3'-methoxyphenoxy) ethyl 1] -N obtained in this way. methyl-diethylaminoacetamide forms a colorless 01 boiling below 0.06 mm at 157-158.



   The new amide is to be used as a local anesthetic and as an intermediate product.



   SUBClaim:
Process according to patent claim, characterized in that an N- [2- (3'-methoxy phenoxy) ethyl-1] -N-methyl-haloacetamide is allowed to react with diethylamine.

** WARNING ** End of DESC field could overlap beginning of CLMS **.



 

Claims (1)

**WARNUNG** Anfang CLMS Feld konnte Ende DESC uberlappen **. ** WARNING ** Beginning of CLMS field could overlap end of DESC **. Verfahren zur Herstellung eines neuen basisch substituierten Fettsäureamides. Process for the production of a new basic substituted fatty acid amide. Gegenstand des vorliegenden Patentes bil clet ein Verfahren zur Herstellung eines neuen basiseh substituierten Fettsäureamides, welches dadureh gekennzeichnet ist, dass man eine Verbindung der Formel EMI1.1 in welcher X einen reaktionsfähigen, während der Reaktion sich abspaltenden Rest bedeutet, mit Diäthylamin umsetzt. The subject of the present patent bil clet a process for the preparation of a new basic substituted fatty acid amide, which is characterized by the fact that a compound of the formula EMI1.1 in which X is a reactive radical which is split off during the reaction, is reacted with diethylamine. Der Rest X kann in einem Halogenatom oder einem sonstigen für den Austausch gegen den basischen Rest geeigneten reaktionsfähigen Substituenten, wie z. B. einer Alkylsulfonyloxy-oder Arylsulfonyloxygruppe, beste hen. Der Austausch der Gruppe X gegen den Diäthylaminrest erfolgt z. B. durch einfaches Erwärmen mit Diäthylamin, gegebenenfalls in Gegenwart eines basisch reagierenden Kondensationsmittels, oder von Diäthylamin im Überschuss. Das N- [2- (3'-Methoxy-phenoxy)- äthyl-1]-N-methyl-diäthylaminoaeetamid ist ein farbloses, unter 0,06 mm bei 157-158 siedendes 01. The radical X can be in a halogen atom or any other reactive substituent suitable for replacement with the basic radical, such as. B. an alkylsulfonyloxy or arylsulfonyloxy group, best hen. The exchange of group X against the diethylamine residue takes place z. B. by simply heating with diethylamine, optionally in the presence of a basic condensing agent, or diethylamine in excess. The N- [2- (3'-methoxyphenoxy) - ethyl-1] -N-methyl-diethylaminoaetamide is a colorless oil that boils below 0.06 mm at 157-158. Das neue Amid soll als Lokalanästhetikum und als Zwischenprodukt zur Herstellung weiterer Derivate Verwendung finden. The new amide will be used as a local anesthetic and as an intermediate for the production of other derivatives. Beispiel : 25,8 g N- [2- (3'-Methoxy-phenoxy)-äthyl-1]- N-methyl-ehloraeeta, mid und 22 g Diäthylamin werden zusammen in 150 mS abs. Benzol 6 Stunden auf dem Wasserbad erhitzt. Das Re aktionsgemisch h wird mit Wasser ausgeschüt- telt und dann mit 2n-Salzsäure ausgezogen. Example: 25.8 g of N- [2- (3'-methoxyphenoxy) ethyl-1] - N-methyl-ehloraeeta, mid and 22 g of diethylamine are dissolved together in 150 mS abs. Benzene heated on a water bath for 6 hours. The reaction mixture h is extracted by shaking with water and then extracted with 2N hydrochloric acid. Darauf wird der salzsaure Auszug mit Äther extrahiert, unter Eiskühlung mit konz. Natronlauge versetzt und das ausgesehiedene öl in Äther aufgenommen. Nach dem Trocknen der Ätherauszüge über Pottasche wird der Äther verdampft und der Rüekstand im Hochvakuum destilliert. The hydrochloric acid extract is then extracted with ether, with conc. Sodium hydroxide solution is added and the separated oil is absorbed in ether. After the ether extracts have dried over potash, the ether is evaporated and the residue is distilled in a high vacuum. Dabei gewinnt man das unter 0,06 min bei 157-158 siedende N- [2- (3'-Methoxy-phen oxy)-äthyl-1]-N-methyl-diäthylaminoacetamid als farbloses, säurelösliches 01. The N- [2- (3'-methoxyphenoxy) -ethyl-1] -N-methyl-diethylaminoacetamide, which boils at 157-158 for less than 0.06 minutes, is obtained as colorless, acid-soluble oil. PATENTANSPRUCH : Verfahren zur Herstellung eines neuen basisch substituierten Fettsäureamides, da dureh gekennzeichnet, dass man eine Verbindung der Formel EMI1.2 in welcher X einen reaktionsfähigen, wahrend der Reaktion sich abspaltenden Rest bedeutet, mit Diäthylamin umsetzt. Das auf diese Weise erhaltene N- [2- (3'-Methoxy-phenoxy)-äthyl 1]-N. methyl-diäthylaminoacetamid bildet ein farbloses, unter 0,06 mm bei 157-158 siedendes 01. PATENT CLAIM: Process for the preparation of a new basic substituted fatty acid amide, characterized by the fact that one is a compound of the formula EMI1.2 in which X is a reactive radical which is split off during the reaction, reacts with diethylamine. The N- [2- (3'-methoxyphenoxy) ethyl 1] -N obtained in this way. methyl-diethylaminoacetamide forms a colorless 01 boiling below 0.06 mm at 157-158. Das neue Amid soll als Lokalanästhetikum und als Zwisehenprodukt Verwendung finden. The new amide is to be used as a local anesthetic and as an intermediate product. UNTERANSPRUCH : Verfahren nach Patentanspruch, dadurch gekennzeichnet, dass man ein N- [2- (3'-Methoxy phenoxy)-äthyl-1]-N-methyl-halogen-acetamid mit Diäthylamin reagieren lässt. SUBClaim: Process according to patent claim, characterized in that an N- [2- (3'-methoxy phenoxy) ethyl-1] -N-methyl-haloacetamide is allowed to react with diethylamine.
CH311678D 1952-06-08 1952-06-08 Process for the production of a new basic substituted fatty acid amide. CH311678A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH311678T 1952-06-08
CH307799T 1952-11-25

Publications (1)

Publication Number Publication Date
CH311678A true CH311678A (en) 1955-11-30

Family

ID=25735411

Family Applications (1)

Application Number Title Priority Date Filing Date
CH311678D CH311678A (en) 1952-06-08 1952-06-08 Process for the production of a new basic substituted fatty acid amide.

Country Status (1)

Country Link
CH (1) CH311678A (en)

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