CH104677A - Process for the preparation of p.oxy-amylphenylmethylamine. - Google Patents

Process for the preparation of p.oxy-amylphenylmethylamine.

Info

Publication number
CH104677A
CH104677A CH104677DA CH104677A CH 104677 A CH104677 A CH 104677A CH 104677D A CH104677D A CH 104677DA CH 104677 A CH104677 A CH 104677A
Authority
CH
Switzerland
Prior art keywords
ether
base
acid
vinegar
amylphenylmethylamine
Prior art date
Application number
Other languages
German (de)
Inventor
Flora Chemische Fabrik
Original Assignee
Chem Fab Flora
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 Chem Fab Flora filed Critical Chem Fab Flora
Publication of CH104677A publication Critical patent/CH104677A/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/08Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C215/48Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups
    • C07C215/50Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups with amino groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/18Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters

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

Description

  

  Verfahren zur Herstellung von p     #        Ogy-amylphenylmethylamin.       p .     Oxy-amylphenylmethylamin    von der       Formel     
EMI0001.0005     
    ist bis jetzt nicht bekannt.

   Es wurde nun  gefunden,     da.ss,    wenn man das Kondensations  produkt aus     Leu,cinäthylester    mit Anisalde  <B>hyd</B> ! mit     Natriumamalgam        reduziert,    völlig  verseift, mit     Mineralsäure    die p .     Methoxy-          benzyl-a-Aminobutylessigsäure    ausfällt, diese  durch Erhitzen in das p .     Methoxy-a@myl-          phenylmethylamin    überführt und aus diesem  Körper die     Methylgruppe    durch Kochen mit       Bromwasserstoffsäure    abspaltet, der ,gesuchte       Körper    entsteht.

    
EMI0001.0018     
    wird ,gewaschen und getrocknet und gibt       beim    Erhitzen auf zirka 200' glatt die       p.Methoxy-amylphenylmetliylaminbase.    Nun  mehr wird die     Methylgruppe    aus dem     Me-          thoxylrest    durch dreistündiges Kochen     mit.     der dreifachen Menge konzentrierter Brom  wasserstoffsäure abgespalten.         Beispiel:     90     gr        Leucinäthylester    werden mit 81     gr     Anisaldehyd versetzt. Die Mischung er  wärmt sich, und es tritt     Wasserabscheidung     ein.

   Das trübe     Reaktionsgemisch        wird    mit  400     gr    Alkohol versetzt und     portionen-          weise    mit 850     gr    8     %igem        Natriumamalgam     reduziert. Das Gemisch wird     alsdann    noch  zirka     '/2    Stunde auf     denn        Wasserbacl    erwärmt  bis zur vollständigen     Verseifung.    Darauf  wird mit     Mineralsäure,    genau neutralisiert.  



  Die abgeschiedene p .     Methoxy-benzyl-a-          Aminobutylessigsäure    von der     Formel       Beim Erkalten erstarrt die Lösung zu  einem     Kristallbrei,    der     abgenutscht    und aus  Wasser umkristallisiert wird.

   Das p .     Oxy-          am.ylphenylmethylaminbromhydrat        schmilzt     bei 152  , Die Analyse ergab folgendes Re  sultat:  
EMI0001.0052     
  
    Brom <SEP> berechnet: <SEP> 29,1
<tb>  Brom <SEP> .gefunden: <SEP> 28,9         Aus der wässerigen Lösung des     Bromhydra-          tes        wird    die freie Base durch Zusatz von  Ammoniak gefällt. Die Base ist unlöslich in  Wasser, sehr leicht löslich in Alkohol, Äther  und Essigäther. Sie kann aus einem Gemenge  von Benzol und     Essigäther        in    Form von wei  ssen Blättchen vom Schmelzpunkt 73' bis 74  erhalten werden.



  Process for the preparation of p # Ogy-amylphenylmethylamine. p. Oxy-amylphenylmethylamine of the formula
EMI0001.0005
    is not yet known.

   It has now been found that if the condensation product of leu, cinethylester with anisalde <B> hyd </B>! reduced with sodium amalgam, completely saponified, with mineral acid the p. Methoxybenzyl-a-aminobutyl acetic acid precipitates, which is transferred to the p. Methoxy-a @ myl-phenylmethylamine is transferred and the methyl group is split off from this body by boiling with hydrobromic acid, which creates the body we are looking for.

    
EMI0001.0018
    is, washed and dried and gives the p.Methoxy-amylphenylmetliylaminbase when heated to about 200 '. The methyl group is now more from the methoxyl residue by boiling for three hours with. split off three times the amount of concentrated hydrobromic acid. Example: 90 g of leucine ethyl ester are mixed with 81 g of anisaldehyde. The mixture warms up and water separates out.

   The cloudy reaction mixture is mixed with 400 grams of alcohol and reduced in portions with 850 grams of 8% sodium amalgam. The mixture is then heated to water for about 1/2 hour until saponification is complete. Then it is precisely neutralized with mineral acid.



  The secluded p. Methoxy-benzyl-a-aminobutyl acetic acid of the formula When it cools, the solution solidifies to form a slurry of crystals that is suction filtered and recrystallized from water.

   The p. Oxy-am.ylphenylmethylamine bromohydrate melts at 152, the analysis gave the following result:
EMI0001.0052
  
    Bromine <SEP> calculated: <SEP> 29.1
<tb> Bromine <SEP>. found: <SEP> 28.9 The free base is precipitated from the aqueous solution of the bromine hydrate by adding ammonia. The base is insoluble in water, very easily soluble in alcohol, ether and vinegar ether. It can be obtained from a mixture of benzene and vinegar ether in the form of white flakes with a melting point of 73 to 74.

 

Claims (1)

PATENTANSPRUCH: Verfahren zur Darstellung von p . OYy- a_uiy lphenylmethylamin, dadurch gekenn- zeiehnet, dass man das Kondensationsprodukt aus Leucinäthylester mit Anisaldehyd mit Natriumamalgam reduziert, völlig verseift, mit Mineralsäure die p.lVletlioxy-benzyl-a-Amino- butylessigsä.ure ausfällt, diese durch Erhit zen in das p . PATENT CLAIM: Method for the representation of p. OYy- a_uiy lphenylmethylamine, characterized in that the condensation product of leucine ethyl ester with anisaldehyde is reduced with sodium amalgam, completely saponified, the p.lVletlioxy-benzyl-a-aminobutyl acetic acid is precipitated with mineral acid, this is zen by heating . llef.hovya.mylphenylmethyl- amin überführt und aus diesem Körper die lletliylgruppe durch Kochen mit Bro,mwasser- stoffsäure abspaltet. llef.hovya.mylphenylmethyl- amine and the lletliyl group is split off from this body by boiling with hydrochloric acid. Aus. dem bromwasser- stoffsauren Salz wird die Base durch Fällen mit Ammoniali: erhalten. Die Base ist un löslich in Wasser, sehr leicht löslich in Al kohol, Äther und Essigäther und kann aus einem Gemenge von Benzol mit Essigäther in Form weisser Blättchen vom SchmelzpunlLt <B>73'</B> bis 74' erhalten werden. Das Produkt soll pha.ima.zeutische Verwendung finden. Out. The base of the hydrobromic acid salt is obtained by precipitation with ammonia. The base is insoluble in water, very easily soluble in alcohol, ether and vinegar ether and can be obtained from a mixture of benzene with vinegar ether in the form of white flakes with a melting point <B> 73 '</B> to 74'. The product is intended to be used for pharmaceutical purposes.
CH104677D 1923-03-24 1923-03-24 Process for the preparation of p.oxy-amylphenylmethylamine. CH104677A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CH104677T 1923-03-24

Publications (1)

Publication Number Publication Date
CH104677A true CH104677A (en) 1924-05-01

Family

ID=4363544

Family Applications (1)

Application Number Title Priority Date Filing Date
CH104677D CH104677A (en) 1923-03-24 1923-03-24 Process for the preparation of p.oxy-amylphenylmethylamine.

Country Status (1)

Country Link
CH (1) CH104677A (en)

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