CH86314A - Process for the preparation of a readily soluble compound of CC-phenylethylbarbituric acid. - Google Patents

Process for the preparation of a readily soluble compound of CC-phenylethylbarbituric acid.

Info

Publication number
CH86314A
CH86314A CH86314DA CH86314A CH 86314 A CH86314 A CH 86314A CH 86314D A CH86314D A CH 86314DA CH 86314 A CH86314 A CH 86314A
Authority
CH
Switzerland
Prior art keywords
acid
preparation
phenylethylbarbituric
compound
readily soluble
Prior art date
Application number
Other languages
German (de)
Inventor
F Hoffmann- Aktiengesellschaft
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of CH86314A publication Critical patent/CH86314A/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/60Three or more oxygen or sulfur atoms
    • C07D239/62Barbituric acids
    • C07D239/64Salts of organic bases; Organic double compounds

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Saccharide Compounds (AREA)

Description

  

  Verfahren zur Darstellung einer leicht löslichen Verbindung der       CC-phenyläthylbarbitursäure.       Die     CC-dialkyl-    und     CC-arylalkylbarbitur-          säuren    besitzen in kaltem Wasser nur eine  geringe Löslichkeit. Ihre wässerigen Lösun  gen sind daher für Injektionszwecke und der  gleichen nicht geeignet. Um den Anforde  rungen in dieser Richtung zu genügen, hat  man die Säuren in ihre     Natriumsalze    über  geführt.

   Diese Verbindungen haben den       Nachteil,    dass ihre wässerige Lösung stark  alkalisch reagiert und die     Barbitursäure     durch das     hydrolytisch    abgespaltene Alkali  eine Zersetzung erleidet, welche mit einer  erheblichen Einbusse der Wirksamkeit ver  bunden ist.  



  Gegenstand der vorliegenden Erfindung  ist ein Verfahren zur Darstellung einer  leicht löslichen Verbindung der     CC-phenyl-          äthylbarbitursäure,    welches darauf beruht,  dass man auf     CC-phenyläthylbarbitursäi.ire          Dimethylamin    einwirken lässt.  



  Die     ,Verbindung    der     CC-phenyläthyl-          barbitursäure    mit     Dimethylamin    ist ein kri  stallisierter Körper, welcher sich in Wasser,  sowie, im     Gegensatze    zu der     Natriumverbin-          dung    der. entsprechenden Säure, in Alkohol    leicht löst und sich gegenüber dem Aus  gangsmaterial durch eine verstärkte hypno  tische Wirkung auszeichnet. Die wässerigen  Lösungen des     Aminsalzes    sind besonders  bei Gegenwart von Alkohol oder andern       hy.droxylhaltigen    organischen Verbindungen,  wie Glyzerin und dergleichen, haltbar.

   Es  ist daher     möglich,    die     Lösungen    des     Salzesi     auch auf dem Wege der Injektion zur     \Vir-          kung    zu bringen.  



  Das neue     Aminsalz    soll in der Therapie  Verwendung finden.  



  <I>Beispiel:</I>  1 Teil     Phenyläthylbarbitursäure    wird  mit etwas mehr als der berechneten Menge  einer 30     %igen    wässerigen Lösung von     Di-          metbylamin    versetzt. Unter Erwärmung ent  steht eine     sirupöse    Lösung, aus welcher die  Verbindung der     Phenyläthylbarbitursäure     mit     Dimethylamin,    nach dem Einengen im       Vakuum,    auskristallisiert.



  Process for the preparation of a readily soluble compound of CC-phenylethylbarbituric acid. The CC-dialkyl- and CC-arylalkylbarbituric acids have only a low solubility in cold water. Your aqueous solutions are therefore not suitable for injections and the like. In order to meet the requirements in this direction, the acids have been converted into their sodium salts.

   These compounds have the disadvantage that their aqueous solution reacts strongly alkaline and the barbituric acid undergoes decomposition as a result of the hydrolytically split off alkali, which is associated with a considerable loss of effectiveness.



  The present invention relates to a process for the preparation of a readily soluble compound of CC-phenyl-ethylbarbituric acid, which is based on the fact that dimethylamine is allowed to act on CC-phenyläthylbarbituric acid.



  The compound of CC-phenylethylbarbituric acid with dimethylamine is a crystallized body, which is in water and, in contrast to the sodium compound, the. corresponding acid, easily dissolves in alcohol and is characterized by an increased hypnotic effect compared to the starting material. The aqueous solutions of the amine salt are particularly stable in the presence of alcohol or other hydroxyl-containing organic compounds such as glycerine and the like.

   It is therefore possible to make the saline solutions active by injection.



  The new amine salt will be used in therapy.



  <I> Example: </I> 1 part of phenylethylbarbituric acid is mixed with a little more than the calculated amount of a 30% aqueous solution of dimethylamine. When heated, a syrupy solution is created from which the compound of phenylethylbarbituric acid with dimethylamine crystallizes out after concentration in vacuo.

 

Claims (1)

PATENTANSPRUCH; Verfahren zur Darstellung einer leicht löslichen Verbindung der CC-phenyläthyl- barbitursäure. dadurch gekennzeichnet, dass m.an auf CC'-phenylätliylbarbitursäure Di- metli,#-laniin einwirken lässt. PATENT CLAIM; Process for the preparation of a readily soluble compound of CC-phenylethyl barbituric acid. characterized in that m.an allows dimethyl, # - laniine to act on CC'-phenylethylbarbituric acid. Die Verbindung der CC-phenyläthyl- barbitursäure mit Dimethylamin ist ein kri stallisierter Körper, welcher sich in Wasser, sc.tvie, im Gegensatze zu der Natriumverbin- dung der entsprechenden Säure, in Alkohol sehr lciclit löst und sich gegenüber dein Aus gangsmaterial durch eine verstärkte hypno tische -Virhun- auszeichnet. The compound of CC-phenylethylbarbituric acid with dimethylamine is a crystallized body which, in contrast to the sodium compound of the corresponding acid, dissolves very nicely in water, in contrast to the sodium compound of the corresponding acid, and becomes stronger than the starting material hypnotic -Virhun. Die wässerigen Lösungen des Aminsalzes sind besonders bei Gegenwart von Alkohol oder andern hy drozylhaltigen organischen Verbindungen, wie Glyzerin und dergleichen, haltbar. Es ist daher möglich, die Lösungen des Salzes auch auf dem Wege der Injektion zur Wir kung zu bringen. Das neue Aminsalz soll in der Therapie Verwendung finden. The aqueous solutions of the amine salt are particularly stable in the presence of alcohol or other hy drozylhaltigen organic compounds such as glycerine and the like. It is therefore possible to bring the solutions of the salt to effect by injection. The new amine salt will be used in therapy.
CH86314D 1917-08-04 1917-08-04 Process for the preparation of a readily soluble compound of CC-phenylethylbarbituric acid. CH86314A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH84997T 1917-08-04
CH86314T 1917-08-04

Publications (1)

Publication Number Publication Date
CH86314A true CH86314A (en) 1920-08-16

Family

ID=25703411

Family Applications (1)

Application Number Title Priority Date Filing Date
CH86314D CH86314A (en) 1917-08-04 1917-08-04 Process for the preparation of a readily soluble compound of CC-phenylethylbarbituric acid.

Country Status (1)

Country Link
CH (1) CH86314A (en)

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