CH273077A - Process for the preparation of a new derivative of m-aminophenol. - Google Patents

Process for the preparation of a new derivative of m-aminophenol.

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Publication number
CH273077A
CH273077A CH273077DA CH273077A CH 273077 A CH273077 A CH 273077A CH 273077D A CH273077D A CH 273077DA CH 273077 A CH273077 A CH 273077A
Authority
CH
Switzerland
Prior art keywords
butoxy
nitro
group
benzyl
amino
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 CH273077A publication Critical patent/CH273077A/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
    • C07C213/02Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing 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
    • C07C215/74Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C07C215/76Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton of the same non-condensed six-membered aromatic ring

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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     eines    neuen Derivates des     m-Amino-phenols.       Gegenstand des Patentes ist ein Verfah  ren zur Herstellung eines neuen Derivates des  in     .Amino-phenols,    welches dadurch gekenn  zeichnet ist, dass man eine Verbindung der  Formel  
EMI0001.0004     
    worin Z eine durch Reduktion in die     Amino-          gruppe        überführbare    Gruppe und X einen  durch Hydrolyse durch die OB-Gruppe aus  tauschbaren     Substituenten,    wie zum Beispiel  ein Halogenatom, ein     Aeyloxyrest    usw., be  deutet,

   mit einem     hydrolysierenden    Mittel  Und das     Hy        drolysenprodukt    mit einem Re  duktionsmittel behandelt. Der so erhaltene     4-          Amino-2-n-butoxy-benzylalkohol    schmilzt bei  60 bis<B>700</B> unscharf und löst sich leicht in  Methanol und Äthanol. Er bildet ein Chlor  hydrat, das bei 2500 unter Zersetzung schmilzt.  Die neue Verbindung soll als Zwischenpro  dukt Verwendung finden.  



       Beispiel   <I>1:</I>  120 g     4-Nitro-2-n-butoxy-benzylbromid    (F.  59 bis 600) werden mit<B>7G g</B>     Natriumacetat     und 1500     cm3    Eisessig 40 Stunden     Rückfluss     gekocht. Man     trennt    das entstandene     Na-          ti-iumbromid    ab und dampft ein. Der Rück  stand wird heiss mit Benzol ausgezogen, die       Benzollösung    verdampft und der Rückstand  aus     Ligroin        (Kp.40    bis 650) umkristallisiert.

      Ausbeute 65 g     4-Nitro-2-n-butoxy-benzylacetat     vom Schmelzpunkt 60 bis 63o, das sind 59 0/0  der Theorie.  



  10 g     4-Nitro-2-n-butoxy-benzylacetat,    40     cm3     konzentrierter Salzsäure, 60     em3    Wasser und  120     em3        Alkohol    werden 7 Stunden Rück  fluss gekocht. Nach dem Abkühlen wird die  ausgefallene feinkristalline Masse abgesaugt  und aus 70     o/oigem    Äthanol umkristallisiert.  Man erhält 5,6 g     4-Nitro-2-n-butoxy-benzyl-          alkoliol    in Form farbloser Nadeln, die bei 85  bis<B>870</B>     schmelzen.     



  30 g     4-Nitro-2-n-butoxy-benzylalkohol,    ge  löst in 400     cm3        abs.        1Vlethanol,    werden mit 6 g       Raney-Nickel    unter einem Wasserstoffdruck  von 1     at.    3     Stunden    lang bei<B>190</B>     geschüttelt.-          Man    befreit die Lösung vom Katalysator, engt  im Vakuum ein und fällt den     4-Amino-2-n-          butoxy-benzylalkohol    aus     Chloroform-Petrol-          äther    um.  



  Man erhält den neuen Alkohol so in  84     o/oiger    Ausbeute als amorphes Pulver, das  bei 60 bis<B>701)</B>     urischarf    schmilzt und sich  leicht in Äthanol     und    Methanol löst. Das  Chlorhydrat des Amins schmilzt bei 2500       unter    Zersetzung.  



  <I>Beispiel</I>     ,:          4-Nitro-2-n-butoxy-benzylbromidwird        durch     sechsstündiges Kochen     mit        einer    Mischung  von     Dioxan/Wasser    in den     entsprechenden     Alkohol übergeführt und dieser nach den An  gaben im Beispiel 1 reduziert.



  Process for the preparation of a new derivative of m-aminophenol. The subject of the patent is a process for the preparation of a new derivative of. Amino-phenol, which is characterized in that a compound of the formula
EMI0001.0004
    where Z denotes a group which can be converted into the amino group by reduction and X denotes a substituent which can be exchanged by hydrolysis by the OB group, for example a halogen atom, an aeyloxy radical, etc.,

   with a hydrolyzing agent and the hydrolysis product is treated with a reducing agent. The 4-amino-2-n-butoxy-benzyl alcohol thus obtained melts indistinctly at 60 to 700 and dissolves easily in methanol and ethanol. It forms a hydrate of chlorine, which melts at 2500 with decomposition. The new connection is to be used as an intermediate product.



       Example <I> 1: </I> 120 g of 4-nitro-2-n-butoxy-benzyl bromide (F. 59 to 600) are refluxed with <B> 7G g </B> sodium acetate and 1500 cm3 of glacial acetic acid for 40 hours . The sodium bromide formed is separated off and evaporated. The residue is extracted hot with benzene, the benzene solution is evaporated and the residue is recrystallized from ligroin (bp 40 to 650).

      Yield 65 g of 4-nitro-2-n-butoxy-benzyl acetate with a melting point of 60 to 63o, which is 59% of theory.



  10 g of 4-nitro-2-n-butoxy-benzyl acetate, 40 cm3 of concentrated hydrochloric acid, 60 em3 of water and 120 em3 of alcohol are refluxed for 7 hours. After cooling, the precipitated finely crystalline mass is filtered off with suction and recrystallized from 70% ethanol. 5.6 g of 4-nitro-2-n-butoxy-benzylalkoliol are obtained in the form of colorless needles which melt at 85 to 870.



  30 g of 4-nitro-2-n-butoxy-benzyl alcohol, dissolved in 400 cm3 of abs. 1Vlethanol, are shaken with 6 g of Raney nickel under a hydrogen pressure of 1 at. For 3 hours at <B> 190 </B>. The solution is freed from the catalyst, concentrated in vacuo and the 4-amino-2 is precipitated -n-butoxy-benzyl alcohol from chloroform-petroleum ether.



  The new alcohol is thus obtained in 84% yield as an amorphous powder, which melts very sharply at 60 to 701) and dissolves easily in ethanol and methanol. The hydrochloride of the amine melts at 2500 with decomposition.



  <I> Example </I>,: 4-Nitro-2-n-butoxy-benzyl bromide is converted into the corresponding alcohol by boiling for six hours with a mixture of dioxane / water and this alcohol is reduced according to the information in Example 1.

 

Claims (1)

PATENTANSPRUCH: Verfahren zur Herstellung eines neuen Derivates des m-Amino-phenols, dadurch ge- kennzeichnet, dass man eine Verbindung der Formel EMI0002.0004 worin Z eine durch Reduktion in die Amino- gruppe überführbare Gruppe und X einen durch Hydrolyse durch die OH-Gruppe aus tauschbaren Substituenten bedeutet, PATENT CLAIM: Process for the preparation of a new derivative of m-amino-phenol, characterized in that a compound of the formula EMI0002.0004 where Z is a group which can be converted into the amino group by reduction and X is a substituent which can be exchanged by hydrolysis by the OH group, mit einem hydrolysierenden Mittel und das Hy- drolysenprodukt mit einem RedAtionsmittel behandelt. Der so erhaltene 4-Amino-2-n- butoxy-benzylalkohol schmilzt bei 60 bis 700 unscharf und löst sieh leicht in Methanol und Äthanol. Er bildet ein Chlorhydrat, das bei 2500 unter Zersetzung schmilzt. Die neue Ver bindung soll als Zwischenprodid#:t Verwen dung finden. UNTERANSPRÜCHE: 1. treated with a hydrolyzing agent and the hydrolysis product with a reducing agent. The 4-amino-2-n-butoxy-benzyl alcohol thus obtained melts indistinctly at 60 to 700 and dissolves easily in methanol and ethanol. It forms a hydrochloride that melts with decomposition at 2500. The new connection is to be used as an intermediate product #: t. SUBCLAIMS: 1. Verfahren nach Patentanspruch da durch gekennzeichnet, dass man ein 4-Nitro- 2-n-butoxy-benzyllialogenid als Ausgangsstoff verwendet. 2. Verfahren nach Patentanspruch und Unteranspruch 1, dadurch gekennzeichnet, dass man 4-Nitro-2-n-butoxy-benzylbromid verwendet. 3. Verfahren nach Patentansprueli, da durch gekennzeichnet, dass man 4-Nitro 9.-n- butoxy-benzylacetat als Ausgangsstoff ver wendet. 4. Verfahren nach Patentanspruch und den Unteransprüchen 1 und 2, dadurch ge kennzeichnet, dass man als hydrolysierendes Mittel Wasser verwendet.. 5. Process according to patent claim, characterized in that a 4-nitro-2-n-butoxy-benzyl halide is used as the starting material. 2. The method according to claim and dependent claim 1, characterized in that 4-nitro-2-n-butoxy-benzyl bromide is used. 3. The method according to patent claims, characterized in that 4-nitro 9-n-butoxy-benzyl acetate is used as the starting material ver. 4. The method according to claim and the dependent claims 1 and 2, characterized in that water is used as the hydrolyzing agent .. 5. Verfahren naeli Patentanspruch, da durch gekennzeichnet, dass man die Reduk tion der Gruppe Z mit katalytisch angereg tem Wasserstoff vornimmt. Method according to patent claim, characterized in that the reduction of group Z is carried out with catalytically excited hydrogen.
CH273077D 1949-04-30 1949-04-30 Process for the preparation of a new derivative of m-aminophenol. CH273077A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CH273077T 1949-04-30

Publications (1)

Publication Number Publication Date
CH273077A true CH273077A (en) 1951-01-31

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ID=4479076

Family Applications (1)

Application Number Title Priority Date Filing Date
CH273077D CH273077A (en) 1949-04-30 1949-04-30 Process for the preparation of a new derivative of m-aminophenol.

Country Status (1)

Country Link
CH (1) CH273077A (en)

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