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CH311662A - 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
CH311662A
CH311662A CH311662DA CH311662A CH 311662 A CH311662 A CH 311662A CH 311662D A CH311662D A CH 311662DA CH 311662 A CH311662 A CH 311662A
Authority
CH
Switzerland
Prior art keywords
production
diethylamine
methylamide
propyl
acid
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 CH311662A publication Critical patent/CH311662A/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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Description

  

  



  Verfahren zur Herstellung eines neuen basisch substituierten   Fettsäureamides.   



   Gegenstand des vorliegenden Patentes bildet ein Verfahren zur Herstellung eines neuen    basisch substituierten Fettsäureamides, wel-    ches dadurch 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   basisehen    Rest geeigneten   reaktionsfähi-    gen Substitnenten, wie zum Beispiel einer Alkylsulfonyloxy- oder Arylsulfonyloxygruppe, bestehen. Der Austausch der Gruppe X gegen den   Diäthylaminorest    erfolgt zum Beispiel   durch    einfaches Erwärmen mit Diäthylamin. gegebenenfalls in Gegenwart eines basisch reagierenden Kondensationsmittels oder von Diäthylamin im Überschuss. Das   Diäthyl-    aminoessigsäure-N-(3-p-ehor-phenoxy-propyl  2)-methylamid    ist ein   farbloses, mter 0, 01    mm bei 166-168  siedendes Öl.



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



   Beispiel :
27,1 g Chloressigsäure-N-(3-p-chlor-phenodxy-propyl-2)-methylamid und 21, 9   g Diäthvl.-    amin werden zusammen in 200 cmS abs. Ben  zol    4 Stunden auf dem Wasserbad erhitzt.



  Das Reaktionsgemiseh wird mit Wasser ausgeschüttelt und dann mit   2n-Salzsäure    ausgezogen. Darauf wird der salzsaure Auszug mit Äther extrahiert, under Eiskühlung mit konz. Natronlauge versetzt und das usage  schiedene    Öl in Äther aufgenommen. Nach dem Troeknen der   Ätherauszüge    über Pottasche wird der Äther verdampft und der Rückstand im Hochvakuum destilliert.



   Dabei gewinnt man das unter 0, 01 mm bei   166-168     siedende   Diäthylaminoessigsäure-N-      (3-p-ehlor-phenoxy-propyl-2)-methylamid    in einer Ausbeute von   750/o    der Theorie. Farbloses Öl, schwer löslich in Wasser, gut in organischen Lösungsmitteln und in   verdünn-    ten Mineralsäuren.  



   PATENTANSPRUCH :
Verfahren zur Herstellung eines   neuve    basisch substituierten   Fettsäureamides,    da  dureh      gekennzeiehnet,    dass man eine   Verbin-    dung der Formel
EMI1.2     
 in welcher X einen reaktionsfähigen, während der Reaktion sieh abspaltenden Rest bedeu  tet,    mit Diäthylamin umsetzt. Das auf diese Weise erhaltene Diäthylaminoessigsäure-N-(3 

**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 is a process for the production of a new basic substituted fatty acid amide, which is characterized in 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 remainder of X can be in a. Halogen atom or another reactive substituent suitable for replacement with the basic radical, such as an alkylsulfonyloxy or arylsulfonyloxy group. Group X is exchanged for the diethylamino radical, for example, by simply heating with diethylamine. optionally in the presence of a basic condensing agent or of diethylamine in excess. The diethylaminoacetic acid N- (3-p-ehor-phenoxy-propyl 2) -methylamide is a colorless oil which boils at 166-168 mter 0.01 mm.



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



   Example:
27.1 g of chloroacetic acid-N- (3-p-chloro-phenodxy-propyl-2) -methylamide and 21.9 g diethvl-amine are dissolved together in 200 cmS abs. Ben zol heated on a water bath for 4 hours.



  The reaction mixture is extracted with water and then extracted with 2N hydrochloric acid. The hydrochloric acid extract is then extracted with ether, while cooling with ice with conc. Sodium hydroxide solution was added and the oil used was added to 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-p-chloro-phenoxy-propyl-2) -methylamide, boiling below 0.01 mm at 166-168, is obtained in a yield of 750% of theory. Colorless oil, sparingly soluble in water, good in organic solvents and in dilute mineral acids.



   PATENT CLAIM:
Process for the production of a newly basic substituted fatty acid amide, because it is marked dureh that one is a compound of the formula
EMI1.2
 in which X means a reactive residue that is split off during the reaction, with diethylamine. The diethylaminoacetic acid N- (3

** 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 bildet ein Verfahren zur Herstellung eines neuen basisch substituierten Fettsäureamides, wel- ches dadurch 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 is a process for the production of a new basic substituted fatty acid amide, which is characterized in 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 basisehen Rest geeigneten reaktionsfähi- gen Substitnenten, wie zum Beispiel einer Alkylsulfonyloxy- oder Arylsulfonyloxygruppe, bestehen. Der Austausch der Gruppe X gegen den Diäthylaminorest erfolgt zum Beispiel durch einfaches Erwärmen mit Diäthylamin. gegebenenfalls in Gegenwart eines basisch reagierenden Kondensationsmittels oder von Diäthylamin im Überschuss. Das Diäthyl- aminoessigsäure-N-(3-p-ehor-phenoxy-propyl 2)-methylamid ist ein farbloses, mter 0, 01 mm bei 166-168 siedendes Öl. The remainder of X can be in a. Halogen atom or another reactive substituent suitable for replacement with the basic radical, such as an alkylsulfonyloxy or arylsulfonyloxy group. Group X is exchanged for the diethylamino radical, for example, by simply heating with diethylamine. optionally in the presence of a basic condensing agent or of diethylamine in excess. The diethylaminoacetic acid N- (3-p-ehor-phenoxy-propyl 2) -methylamide is a colorless oil which boils at 166-168 mter 0.01 mm. 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 : 27,1 g Chloressigsäure-N-(3-p-chlor-phenodxy-propyl-2)-methylamid und 21, 9 g Diäthvl.- amin werden zusammen in 200 cmS abs. Ben zol 4 Stunden auf dem Wasserbad erhitzt. Example: 27.1 g of chloroacetic acid-N- (3-p-chloro-phenodxy-propyl-2) -methylamide and 21.9 g diethvl-amine are dissolved together in 200 cmS abs. Ben zol heated on a water bath for 4 hours. Das Reaktionsgemiseh wird mit Wasser ausgeschüttelt und dann mit 2n-Salzsäure ausgezogen. Darauf wird der salzsaure Auszug mit Äther extrahiert, under Eiskühlung mit konz. Natronlauge versetzt und das usage schiedene Öl in Äther aufgenommen. Nach dem Troeknen der Ätherauszüge über Pottasche wird der Äther verdampft und der Rückstand 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 ether, while cooling with ice with conc. Sodium hydroxide solution was added and the oil used was added to 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, 01 mm bei 166-168 siedende Diäthylaminoessigsäure-N- (3-p-ehlor-phenoxy-propyl-2)-methylamid in einer Ausbeute von 750/o der Theorie. Farbloses Öl, schwer löslich in Wasser, gut in organischen Lösungsmitteln und in verdünn- ten Mineralsäuren. The diethylaminoacetic acid N- (3-p-chloro-phenoxy-propyl-2) -methylamide, boiling below 0.01 mm at 166-168, is obtained in a yield of 750% of theory. Colorless oil, sparingly soluble in water, good in organic solvents and in dilute mineral acids. PATENTANSPRUCH : Verfahren zur Herstellung eines neuve basisch substituierten Fettsäureamides, da dureh gekennzeiehnet, dass man eine Verbin- dung der Formel EMI1.2 in welcher X einen reaktionsfähigen, während der Reaktion sieh abspaltenden Rest bedeu tet, mit Diäthylamin umsetzt. Das auf diese Weise erhaltene Diäthylaminoessigsäure-N-(3 p-chlor-phenoxy-propyl-2)-methylamid bildet ein farboses, unter 0,01 mm bei 166-168 siedendes Öl. PATENT CLAIM: Process for the production of a newly basic substituted fatty acid amide, because it is marked dureh that one is a compound of the formula EMI1.2 in which X means a reactive residue that is split off during the reaction, with diethylamine. The diethylaminoacetic acid N- (3-chloro-phenoxy-propyl-2) -methylamide obtained in this way forms a colorless oil boiling below 0.01 mm at 166-168. 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 nach patentanspruch, dadurch gekennzeichnet, dass man ein Halogenessig- säure-N- (3-p-chlor-phenoxy-propyl-2)-methylamid mit Diäthylamin reagieren lässt. SUBClaim: Process according to claim, characterized in that a haloacetic acid-N- (3-p-chloro-phenoxy-propyl-2) -methylamide is allowed to react with diethylamine.
CH311662D 1952-06-08 1952-06-08 Process for the production of a new basic substituted fatty acid amide. CH311662A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH311662T 1952-06-08
CH307799T 1952-11-25

Publications (1)

Publication Number Publication Date
CH311662A true CH311662A (en) 1955-11-30

Family

ID=25735395

Family Applications (1)

Application Number Title Priority Date Filing Date
CH311662D CH311662A (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) CH311662A (en)

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