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CH311664A - 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.

Info

Publication number
CH311664A
CH311664A CH311664DA CH311664A CH 311664 A CH311664 A CH 311664A CH 311664D A CH311664D A CH 311664DA CH 311664 A CH311664 A CH 311664A
Authority
CH
Switzerland
Prior art keywords
diethylamine
acid
new
production
amide
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 CH311664A publication Critical patent/CH311664A/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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Description

  

  



  Verfahren zur Herstellung eines neuen basisch substituierten FettsÏureamides.



   Gegenstand des vorliegenden Patentes bil. (let   ein Verfahren zur Herstellung eines neuen    basisch substituierten FettsÏureamides, wel   c-lies dadureh gekennzeiehnet ist, dass man    c-ine Verbindung der Formel
EMI1.1     
 in welcher   X    einen reaktionsfähigen, während der Reaktion sich abspaltenden Rest becleutet, mit Diäthylamin umsetzt.



   Der Rest X kann in einem Halogenatom     der einem    sonstigen für den   Austauseh    gegen den   basisehen Rest geeigneten reaktionsfähi-    gen Snbstituenten, wie zum Beispiel einer.   @l-    kylsulfonyloxy- oder Arysulfonyloxygruppe,   hestehen. Der Austauseh    der Gruppe X gegen den   Diäthylaminorest erfolgt zum    Beispiel   durch einfaches Erwärmen    mit Diäthylamin, gegebenenfalls in Gegenwart eines basisch reagierenden Kondensationsmittels oder von DiÏthylamin im ¯berschu¯. Das   Diäthyl-       !) minoessigsaure-N- (3-o-chlor-phenoxy-propyl-    2)-Ïthylamid ist ein farbloses, unter 0, 06 mm bei 110-112¯ siedendes   61.   



   Das neue Amid soll als   Lokalanästhetikum    und als Zwischenprodukt zur Herstellung   v-eiterer Derivate Verwendung finden.   



   Beispiel :    29,    0 g ChloressigsÏure-N-(3-o-Chlor-phenoxy-propyl-2)-Ïthylamid und 15, 5 g Diäthylamin werden zusammen in 200 cm3 abs. Benzol 3 Stunden   aul    dem Wasserbad erhitzt.



  Das Reaktionsgemisch wird mit Wasser ausgeschüttelt und dann mit   2n-Salzsäure    ausgezogen. Darauf wird der salzsaure Auszug mit ¯ther extrahiert, unter   Eiskühlung    mit konz. Natronlauge versetzt und das ausge  sehiedene      61    in Äther aufgenommen. Nach dem Trocknen der Atherauszüge  ber Pottasehe wird der ¯ther verdampft und der Riiekstand im Hochvakuum destilliert.



   Dabei gewinnt man das unter 0, 06 mm bei 110-112  siedende   Diä, thylaminoessigsäure-N-    (3-o-chlor-phenoxy-propyl-2)-Ïthylamid in einer Ausbeute von 56%der Theorie. Farbloses   öl,    sehwer   löslieh    in Wasser, gut in organischen   Losungsmitteln    und in   verdünn-    ten Mineralsäuren.  



   PATENTANSPRUCH :
Verfahren zur   I3erstellung    eines neuen basisch substituierten   Fettsäureamides,    dadurch gekennzeichnet, dass man eine   Verbin-      dung    der Formel
EMI1.2     
 in welcher X einen reaktionsfähigen, während der Reaktion sieh   abspaltenden    Rest bedeutet, mit   Diathylamin    umsetzt. Das auf diese Weise    erlialtene Diathylaminoessigsäure-N- (3-o-ehlor-    

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





  



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



   Subject of the present patent bil. (Let a process for the production of a new basic substituted FettsÏureamides, wel c-lies because it is marked that one c-a compound of the formula
EMI1.1
 in which X reacts a reactive residue which is split off during the reaction with diethylamine.



   The radical X can be in a halogen atom of another reactive substituent suitable for exchange with the basic radical, for example one. @ l-kylsulfonyloxy or arysulfonyloxy group. Group X is exchanged for the diethylamino radical, for example, by simply heating with diethylamine, if appropriate in the presence of a basic condensing agent or an excess of diethylamine. The diethyl-!) Minoacetic acid-N- (3-o-chloro-phenoxy-propyl-2) -thylamide is a colorless 61 that boils below 0.06 mm at 110-112¯.



   The new amide is to be used as a local anesthetic and as an intermediate for the production of v-pus derivatives.



   Example: 29.0 g of chloroacetic acid-N- (3-o-chloro-phenoxy-propyl-2) -thylamide and 15.5 g of diethylamine are combined in 200 cm3 of abs. Benzene heated on a water bath for 3 hours.



  The reaction mixture is extracted with water and then extracted with 2N hydrochloric acid. The hydrochloric acid extract is then extracted with ¯ther, with ice cooling with conc. Sodium hydroxide solution was added and the separated 61 was taken up in ether. After the ether extracts have dried over potash, the ether is evaporated and the residue is distilled in a high vacuum.



   The diethylaminoacetic acid-N- (3-o-chlorophenoxy-propyl-2) -thylamide boiling below 0.06 mm at 110-112 is obtained in a yield of 56% of theory. Colorless oil, very soluble in water, good in organic solvents and in dilute mineral acids.



   PATENT CLAIM:
Process for the preparation of a new, basically substituted fatty acid amide, characterized in that a compound of the formula
EMI1.2
 in which X denotes a reactive radical which is split off during the reaction, with diethylamine. The diethylaminoacetic acid-N- (3-o-ehlor-

** 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 FettsÏureamides. Process for the production of a new basic substituted fatty acid amide. Gegenstand des vorliegenden Patentes bil. (let ein Verfahren zur Herstellung eines neuen basisch substituierten FettsÏureamides, wel c-lies dadureh gekennzeiehnet ist, dass man c-ine Verbindung der Formel EMI1.1 in welcher X einen reaktionsfähigen, während der Reaktion sich abspaltenden Rest becleutet, mit Diäthylamin umsetzt. Subject of the present patent bil. (Let a process for the production of a new basic substituted FettsÏureamides, wel c-lies because it is marked that one c-a compound of the formula EMI1.1 in which X reacts a reactive residue which is split off during the reaction with diethylamine. Der Rest X kann in einem Halogenatom der einem sonstigen für den Austauseh gegen den basisehen Rest geeigneten reaktionsfähi- gen Snbstituenten, wie zum Beispiel einer. @l- kylsulfonyloxy- oder Arysulfonyloxygruppe, hestehen. Der Austauseh der Gruppe X gegen den Diäthylaminorest erfolgt zum Beispiel durch einfaches Erwärmen mit Diäthylamin, gegebenenfalls in Gegenwart eines basisch reagierenden Kondensationsmittels oder von DiÏthylamin im ¯berschu¯. Das Diäthyl- !) minoessigsaure-N- (3-o-chlor-phenoxy-propyl- 2)-Ïthylamid ist ein farbloses, unter 0, 06 mm bei 110-112¯ siedendes 61. The radical X can be in a halogen atom of another reactive substituent suitable for exchange with the basic radical, for example one. @ l-kylsulfonyloxy or arysulfonyloxy group. Group X is exchanged for the diethylamino radical, for example, by simply heating with diethylamine, if appropriate in the presence of a basic condensing agent or an excess of diethylamine. The diethyl-!) Minoacetic acid-N- (3-o-chloro-phenoxy-propyl-2) -thylamide is a colorless 61 that boils below 0.06 mm at 110-112¯. Das neue Amid soll als Lokalanästhetikum und als Zwischenprodukt zur Herstellung v-eiterer Derivate Verwendung finden. The new amide is to be used as a local anesthetic and as an intermediate for the production of v-pus derivatives. Beispiel : 29, 0 g ChloressigsÏure-N-(3-o-Chlor-phenoxy-propyl-2)-Ïthylamid und 15, 5 g Diäthylamin werden zusammen in 200 cm3 abs. Benzol 3 Stunden aul dem Wasserbad erhitzt. Example: 29.0 g of chloroacetic acid-N- (3-o-chloro-phenoxy-propyl-2) -thylamide and 15.5 g of diethylamine are combined in 200 cm3 of abs. Benzene heated on a water bath for 3 hours. Das Reaktionsgemisch wird mit Wasser ausgeschüttelt und dann mit 2n-Salzsäure ausgezogen. Darauf wird der salzsaure Auszug mit ¯ther extrahiert, unter Eiskühlung mit konz. Natronlauge versetzt und das ausge sehiedene 61 in Äther aufgenommen. Nach dem Trocknen der Atherauszüge ber Pottasehe wird der ¯ther verdampft und der Riiekstand im Hochvakuum destilliert. The reaction mixture is extracted with water and then extracted with 2N hydrochloric acid. The hydrochloric acid extract is then extracted with ¯ther, with ice cooling with conc. Sodium hydroxide solution was added and the separated 61 was taken up 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 mm bei 110-112 siedende Diä, thylaminoessigsäure-N- (3-o-chlor-phenoxy-propyl-2)-Ïthylamid in einer Ausbeute von 56%der Theorie. Farbloses öl, sehwer löslieh in Wasser, gut in organischen Losungsmitteln und in verdünn- ten Mineralsäuren. The diethylaminoacetic acid-N- (3-o-chlorophenoxy-propyl-2) -thylamide boiling below 0.06 mm at 110-112 is obtained in a yield of 56% of theory. Colorless oil, very soluble in water, good in organic solvents and in dilute mineral acids. PATENTANSPRUCH : Verfahren zur I3erstellung eines neuen basisch substituierten Fettsäureamides, dadurch gekennzeichnet, dass man eine Verbin- dung der Formel EMI1.2 in welcher X einen reaktionsfähigen, während der Reaktion sieh abspaltenden Rest bedeutet, mit Diathylamin umsetzt. Das auf diese Weise erlialtene Diathylaminoessigsäure-N- (3-o-ehlor- phenoxy-propyl-2)-äthylamid bildet ein farbloses, unter 0, 06 mm bei 110-112¯ siedendes 01. PATENT CLAIM: Process for the preparation of a new, basically substituted fatty acid amide, characterized in that a compound of the formula EMI1.2 in which X denotes a reactive radical which is split off during the reaction, with diethylamine. The diethylaminoacetic acid-N- (3-o-chlorophenoxy-propyl-2) -ethylamide obtained in this way forms a colorless oil that boils below 0.06 mm at 110-112¯. Das neue Amid soll als Lokalanästhetikum und als Zwischenprodukt Verwendung finden. The new amide will be used as a local anesthetic and as an intermediate product. UNTERANSPRUCH: Verfahren naeh Patentanspruch, dadurch gekennzeichnet, dass man ein Ha. logenessig sänre-N- (3-o-chlor-phenoxy-propy)-2)-äthy]- amid mit Diäthylamin reagieren lässt. SUBClaim: Method according to patent claim, characterized in that a Ha. logenessig acid-N- (3-o-chloro-phenoxy-propy) -2) -ethy] - amide reacts with diethylamine.
CH311664D 1952-06-08 1952-06-08 Process for the production of a new basic substituted fatty acid amide. CH311664A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH311664T 1952-06-08
CH307799T 1952-11-25

Publications (1)

Publication Number Publication Date
CH311664A true CH311664A (en) 1955-11-30

Family

ID=25735397

Family Applications (1)

Application Number Title Priority Date Filing Date
CH311664D CH311664A (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) CH311664A (en)

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