CH86317A - Process for the preparation of a readily soluble compound of CC diethylbarbituric acid. - Google Patents

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

Info

Publication number
CH86317A
CH86317A CH86317DA CH86317A CH 86317 A CH86317 A CH 86317A CH 86317D A CH86317D A CH 86317DA CH 86317 A CH86317 A CH 86317A
Authority
CH
Switzerland
Prior art keywords
acid
preparation
readily soluble
compound
diethylbarbituric acid
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 CH86317A publication Critical patent/CH86317A/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

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

Description

  

  Verfahren zur Darstellung einer leicht löslichen Verbindung der     CC-diäthylbarbitursäure.       Die     CC-dialkyl-    und     CC-arylalliylbarbitur-          säuren    besitzen in kaltem Wasser nur eine  geringe     Löslichkeit.    Ihre wässerigen Lösun  gen sind daher für     Injektionszwecske    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     finit    einer  erheblichen Einbusse der     Wirksamkeit    ver  bunden ist.  



  Gegenstand der vorliegenden Erfindung  ist ein Verfahren zur Darstellung einer  leicht löslichen Verbindung der     CC-di-          äthylbarbitursäure,    welches darauf beruht,  dass man auf     CC-diäthylbarbitursäure        Cholin     einwirken lässt.  



  Die Verbindung der     CC-diäthylbar-          bitursäure    mit     Cholin    ist ein geruchloser,  kristallisierter Körper, welcher sich in     Wasser,          sowie,    im     Gegensatze    zu der     Natriuniverbin        -          dung    der entsprechenden Säure, in     All:

  oliol          leicht    löst und sich gegenüber denn Aus.-         gangsinaterial    durch eine     verstiirkte        hypno-          tische        Wirkung    auszeichnet.

   Die     wässeri-en          Lösungen    des     Aminsalzes    sind besonders       hei    Gegenwart von Alkohol oder     andern          hydrozyllialtigen    organischen     Verbi.nditno,eil,     wie     Glyzerin    und     dergleichen,        lia.ltb@ir.    Es  ist daher möglich, die     Lö        sun-en    des     S@ilz,@s          a,ueh    auf dein Wege der Injektion     zur    Wir  kung zu     bringen.     



  Das neue     Aminsalz    soll in der     Therapie     Verwendung finden.  



  <I>Beispiel:</I>  184,2 Teile     Diäthvlbarbitursäure    werden  unter Rühren eingetragen in     666-"/"        Rauan-          teile    einer     1J_    normalen     Cholinlösung    bei.

         Zimmertemperatur.    Die     entstehende        Lösung     wird filtriert und liefert alsdann beim Ein  trocknen unter     stank    vermindertem Druck  eine weisse kristallinische     Masse,    die     das          Cholinsalz    der     Diäthylbarbitursä        .ure        darstellt.     Die Verbindung     isty    geruchlos und äusserst  leicht löslich in Wasser     finit        alkalischer     Reaktion.



  Process for the preparation of a readily soluble compound of CC diethylbarbituric acid. The CC-dialkyl and CC-arylalliylbarbituric acids have only a low solubility in cold water. Your aqueous solutions are therefore not suitable for injection purposes 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 finitely linked to a considerable loss of effectiveness.



  The present invention relates to a method for the preparation of a readily soluble compound of CC diethylbarbituric acid, which is based on the fact that CC diethylbarbituric acid is allowed to act on choline.



  The compound of CC diethylbarbituric acid with choline is an odorless, crystallized body, which is in water, and, in contrast to the sodium compound of the corresponding acid, in space:

  oliol dissolves easily and is distinguished from the starting material by an enhanced hypnotic effect.

   The aqueous solutions of the amine salt are particularly useful in the presence of alcohol or other hydrocyclic organic compounds, such as glycerine and the like, lia.ltb@ir. It is therefore possible to bring the solutions of S @ ilz, @ s a, ueh to effect by means of injection.



  The new amine salt will be used in therapy.



  <I> Example: </I> 184.2 parts of dietary barbituric acid are added to 666 - "/" rough parts of a 1J_ normal choline solution with stirring.

         Room temperature. The resulting solution is filtered and then, when dried under reduced pressure, gives a white crystalline mass which is the choline salt of diethylbarbituric acid. The compound is odorless and extremely easily soluble in water with a finite alkaline reaction.

 

Claims (1)

PATENTANSPRUCH: Verfahren zur Darstellung einer leicht löslichen Verbindung der CC-diä.thylbar- l_;itursäure, dadurch gekennzeichnet, da13 man auf CC-diäthylbarbitursä_ure Cholin ein wirken lärt. Die Verbindung der CC-diäthylba.r- bitursäure reit Cholin ist ein geruchloser. PATENT CLAIM: Process for the preparation of a readily soluble compound of CC-diethylbarbituric acid, characterized in that CC-diethylbarbituric acid choline is acted upon. The compound of CC-diethylba.r-bituric acid reit choline is odorless. 1-,ristallisierter Körper, welcher sich in Wasser, sowie, im Gegensatze zu der Natriumverbin- dung der entsprechenden Säure, in Alkohol sehr leicht löst und sich gegenüber dem Aus gangsmaterial durch eine verstärkte hypno tische Wirkung auszeichnet. Die wässerigen Lösungen des Aminsa.lzes sind besonders bei Gegenwart von Alkohol oder andern hy droxylhaltigen organischen Verbindungen, wie Glyzerin und dergleichen, haltbar. 1-, crystallized body, which dissolves very easily in water and, in contrast to the sodium compound of the corresponding acid, in alcohol and is characterized by an increased hypnotic effect compared to the starting material. The aqueous solutions of Aminsa.lzes are particularly stable in the presence of alcohol or other hy droxyl-containing organic compounds such as glycerine and the like. 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. It is therefore possible to bring the solutions of the salt to effect by injection. The new amine salt will be used in therapy.
CH86317D 1917-08-04 1917-08-04 Process for the preparation of a readily soluble compound of CC diethylbarbituric acid. CH86317A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH84997T 1917-08-04
CH86317T 1917-08-04

Publications (1)

Publication Number Publication Date
CH86317A true CH86317A (en) 1920-08-16

Family

ID=25703414

Family Applications (1)

Application Number Title Priority Date Filing Date
CH86317D CH86317A (en) 1917-08-04 1917-08-04 Process for the preparation of a readily soluble compound of CC diethylbarbituric acid.

Country Status (1)

Country Link
CH (1) CH86317A (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1134679B (en) * 1957-01-31 1962-08-16 Leo Werke G M B H Process for the preparation of a salt of 5-phenyl-5-aethylbarbituric acid
DE1147587B (en) * 1961-08-19 1963-04-25 Leo Werke G M B H Process for the preparation of choline 5-phenyl-5-ethyl barbiturate

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1134679B (en) * 1957-01-31 1962-08-16 Leo Werke G M B H Process for the preparation of a salt of 5-phenyl-5-aethylbarbituric acid
DE1147587B (en) * 1961-08-19 1963-04-25 Leo Werke G M B H Process for the preparation of choline 5-phenyl-5-ethyl barbiturate

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