CH84997A - Process for preparing an easily soluble compound of CC-diethylbarbituric acid. - Google Patents

Process for preparing an easily soluble compound of CC-diethylbarbituric acid.

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Publication number
CH84997A
CH84997A CH84997DA CH84997A CH 84997 A CH84997 A CH 84997A CH 84997D A CH84997D A CH 84997DA CH 84997 A CH84997 A CH 84997A
Authority
CH
Switzerland
Prior art keywords
acid
compound
alcohol
preparing
easily 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 CH84997A publication Critical patent/CH84997A/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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Description

Verfabren zur Dai-stellung einer leicbt lüsliclien Verbindung der CC-diâtliylbarbitur siiur e. Process for the preparation of an easily soluble compound of the CC-diâtliylbarbitur acid e.

Die CC-dialkyl- und CC-arylalkylbarbitur sâuren besitzen in kaltem Wasser nur eine geringe LSslichkeit. Ihre wâsserigen L6sungen sind daher für Injektionszwecke und der gleichen niclit geeignet. Um den Anforderungen in dieser Richtung zu genügen, hat man die Süuren in ihre Natriumsalze übergeführt. Diese Verbindungen haben den Nachteil, dah ihre wâsserige Lbsung stark alkalisch reagiert und die Barbitursàure durch das hydrolytisch abgespaltene Alkali eine Zersetzung erleidet, welche mit einer erheblichen Einbuee der Wirksamkeit verbunden ist. The CC dialkyl and CC arylalkyl barbituric acids have only a low solubility in cold water. Their aqueous solutions are therefore not suitable for injection purposes and the same. 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 has a strongly alkaline reaction and the barbituric acid undergoes decomposition as a result of the hydrolytically split off alkali, which is associated with a considerable loss of effectiveness.

Gegenstand der vorliegenden Erfindung ist ein Verfahren zur Darstellung einer leiclit 16slichen Verbindung der CC-diâthylbarbitur sâure, welches darauf beruht, daG man auf CC-diâ.thylbarbitursâtire Diâthylamin einwir ken lâBt. The subject of the present invention is a process for the preparation of a soluble compound of CC-diâ.thylbarbituric acid, which is based on allowing diethylamine to act on CC-diâ.thylbarbitursâtire.

Die Verbindung der CC-diâthylbarbitur süure mit Diüthylamin ist ein kristallisierter gSrper, welcher sich in Wasser, sowie, im Gegensatze zu der Natriumverbindung der entsprechenden Sâure, in Alkohol sehr leiclit lbst und sich gegenüber dem Ausgangsmaterial The compound of CC-diethylbarbituric acid with diethylamine is a crystallized body which dissolves very easily in water and, in contrast to the sodium compound of the corresponding acid, in alcohol and differs from the starting material

durcli eine verstiirkte hypnotische Wirkung auszeichnet. Die wüsserigen Lüsungen des Aminsalzes sind besonders bei Gegenwart von Alkoliol oder andern hydroxyllialtigen or ganisclien Verbindungen, wie Glyzerin und dergleichen, haltbar. Es ist daller m;3glich, die Lüsungen des Salzes auch auf dem Wege der Injektion zur Wirkung zu bringen. characterized by an increased hypnotic effect. The aqueous solutions of the amine salt are particularly stable in the presence of alcohol or other hydroxylated organic compounds such as glycerine and the like. It is then possible to bring the solutions of the salt into action by way of injection.

Das noue Aininsalz roll in der Therapie Verwendung finden. The noue Aininsalz roll can be used in therapy.

<I>Beispiel 1:</I> 1 Teil Diüthylbarbitursii,ure wird in 1,7 Teilen absolutem Alkohol unter Zugabe von wenig mehr als der theoretisch notwendigen Menge inüglichst hocliprozentigem Diâthylamin bel 50-60 gelüst. Die warme Lüsung wird filtriert und noch warni mit 2,2 Teilen ab solutem ther versetzt. Aus der zuniichst klarbleibenden Lüsung kristallisiert allmühlich die Hauptinenge der neuen Verbindung aus. <I>Beispiel 2</I> 1 Teil inügliehst fein pulverisierte Diâthyl barbitursâure wird mit dem anderthalbfaehen der theoretisch notwendigen Menge Diâthyl- <I>Example 1:</I> 1 part of diethylbarbituric acid is dissolved in 1.7 parts of absolute alcohol with the addition of a little more than the theoretically necessary amount of diethylamine with the highest possible concentration at 50-60. The warm solution is filtered, and 2.2 parts of absolute ether are still added. The bulk of the new compound gradually crystallizes out of the initially clear solution. <I>Example 2</I> 1 part of the most finely powdered diethyl barbituric acid is mixed with one and a half times the theoretically required amount of diethyl

amie innig verrieben. Unter Erwârmung ver flüssigt sich das Reaktionsgemisch zu einem klaren Sirup, der bald erstarrt. Die entstan dene Verbindung der Diâthylbarbitursâure mit Diâthylamin wird durch kurzes Liegen an der Luft voie überschüssigen Diâthylamin getrennt. Sie ist in Wasser sûr leicht, in den üblichen organischen Lüsungsmitteln leiclit lôslich. amie deeply rubbed. When heated, the reaction mixture liquefies to form a clear syrup, which soon solidifies. The resulting compound of diethylbarbituric acid with diethylamine is separated from excess diethylamine by briefly lying in air. It is very easily soluble in water and slightly soluble in the usual organic solvents.

<I>Beispiel 3</I> 1 Teil Diâtliylbarbitursâui-e wird in 6 Teilo einer wasserigen Lüsung, welche 0,4 Telle Diütlivlamin enthült, eingetragen. Die Diâthyl barhI'tui'Sâ,nrB 1iist sich glatt, und die ent standene Lbsung ist, gegeberienfalls nach vorheriger Filtration, <B>zur</B> Verwendung für theraheutische Zwecke gebrauchsfertig. <I>Example 3</I> 1 part of diethylbarbituric acid is added to 6 parts of an aqueous solution containing 0.4 part of diylivlamin. The Diâthyl barhI'tui'Sâ,nrB 1i is smooth and the resulting solution is ready for use, after prior filtration if necessary, <B>for</B> use for therapeutic purposes.

Claims (1)

PATENTANSPRUCH: CLAIM: Verfaliren znr Darstellung einer leicht hislichen Verbindung der CC-didthylbarbitur- Methods for the preparation of a slightly different compound of the CC-didthylbarbitur- saure, dadurch gekennzeichnet, daP man auf CC-diâthylbarbitursâ.ure Diüthvlamin einwir ken lâet. Die Verbindung der CC-diâthy lbarbitur sâure mit Diâthylamin ist ein kristallisierter Kürper, welcher sich in Wasser, sowie, im Gegensatze zu der Natriumverbindung der entsprechenden Saure, in Alkohol sehr leiclit lüst und sich gegenüber dem Ausgangsmaterial durch eine verstârkte hypnotische Wirkung auszeichriet. Die wâsserigen Lôsungen des Aminsalzes sied besonders bel Gegenwart von Alkohol oder andern hydroxylhaltigen organischen Verbindungen, wie Glyzerin und dergleichen, haltbar. Es ist daller môglich, die Lüsungen des Salzes auch auf dem Wege der Injektion zur Wirkung zu bringen. Das lieue Aminsalz roll in der Therapie Verwendung finden. acidic, characterized in that dithvlamin is allowed to act on CC-diâthylbarbituric acid. The compound of CC-diethylbarbituric acid with diethylamine is a crystallized body which, in contrast to the sodium compound of the corresponding acid, 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 the amine salt are particularly stable boiling in the presence of alcohol or other hydroxyl-containing organic compounds such as glycerin and the like. It is then possible to bring the solutions of the salt into action also by injection. The lieue amine salt roll find use in therapy.
CH84997D 1917-08-04 1917-08-04 Process for preparing an easily soluble compound of CC-diethylbarbituric acid. CH84997A (en)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
CH84997A true CH84997A (en) 1920-05-01

Family

ID=4341230

Family Applications (1)

Application Number Title Priority Date Filing Date
CH84997D CH84997A (en) 1917-08-04 1917-08-04 Process for preparing an easily soluble compound of CC-diethylbarbituric acid.

Country Status (1)

Country Link
CH (1) CH84997A (en)

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