DE674241C - Process for the preparation of readily soluble theophylline compounds - Google Patents
Process for the preparation of readily soluble theophylline compoundsInfo
- Publication number
- DE674241C DE674241C DEG84101D DEG0084101D DE674241C DE 674241 C DE674241 C DE 674241C DE G84101 D DEG84101 D DE G84101D DE G0084101 D DEG0084101 D DE G0084101D DE 674241 C DE674241 C DE 674241C
- Authority
- DE
- Germany
- Prior art keywords
- preparation
- readily soluble
- theophylline
- compounds
- theophylline compounds
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
Verfahren zur Herstellung von leicht löslichen Theophyllinverbindungen Das als Diureticum bewährte Theophyllinäthylendiamin hat man bereits (Patentschrift 469 788) in seiner harntreibenden Wirkung dadurch verbessert, daß man es tutter Mitwirkung von salicylsaurem Äthylendiamin mit einer größeren Menge Calciumchlorid vereinigte. Das letztere bleibt dabei als solches beistehen, da das Ca mit der stärksten Säure verbunden bleibt. Auch sind hier mehrere Mole Ca Cl, mit wenig, höchstens 2/3 Mol., Theophyllin vereinigt.Process for the preparation of readily soluble theophylline compounds Theophylline ethylenediamine, which has proven itself as a diuretic, is already available (patent specification 469 788) improves its diuretic effect by tuttering it Contribution of salicylic acid ethylenediamine with a larger amount of calcium chloride united. The latter remains as such, since the Ca with the strongest Acid remains connected. Also here are several moles of Ca Cl, with little, at most 2/3 mol., Theophylline combined.
Es, wurde nun versucht, die Wirkinnig ides Theophyllinäthylendiamins so zu verändern, daß nicht die diuretis.che Wirkung verstärkt, sondern daß .eine Änderung in zentralwirkender s:pasmolytischer Richtung erreicht wird.Attempts have now been made to find the active substance of theophylline ethylenediamine to change so that not the diuretic effect is strengthened, but that one Change in the centrally acting s: pasmolytic direction is achieved.
So wurde gefunden, @daß das aufs i Mol. Theophyllin und i Mol. Äthylendiaminoder etwas mehr hergestellte Theophyllinäthylendiamin imstande ist, bis etwa i/,, Mol. Phenyläthylbarbitursätire aufzulösen. Man erhält Produkte von sehr hoher Löslichkeit, die rektal sehr rasch wirken und zudem auch intravenös und intramuskulär injiziert werden können mit sofort einsetzender Wirkung. Sie sind Gefäßmittel von erhöhter Wirksamkeit.It has been found that this amounts to 1 mole of theophylline and 1 mole of ethylenediamine or a little more produced theophylline ethylenediamine is capable of up to about i / ,, mol. Dissolve Phenyläthylbarbitursätire. Products of very high solubility are obtained, which act very quickly rectally and are also injected intravenously and intramuscularly with immediate effect. They are vascular means of increased Effectiveness.
Zur Herstellung können die Ausgangsstoffe in beliebiger Reihenfolge zusammengebracht werden, mit und ohne Lösiungsmittel, am besten unter schwacher Kühlung, da die Umsetzung unter Wärmeabgabe erfolgt. Ein geringer übersch.uß an Diamin ist zweckdienlich im Hinblick auf die Empfindlichkeit gegenüber der Kohlensäure der Luft.The starting materials can be used in any order for production be brought together, with and without solvents, preferably under weak Cooling, since the conversion takes place with the release of heat. A small excess of Diamine is useful in terms of sensitivity to carbonic acid the air.
Die Pxodukte lösen sich leicht in Wasser, wenig in Alkohol. Durch Alkalien und Säuren werden sie zerlegt, schon durch Kohlensäure. Die festen Produkte sind kristallinisch ohne festen Schmelzpunkt. Beim Schmelzen -und vor .dem Schmelzen spalten sie Amin ab. Geht man von den Komponenten aus in Anwesenheit von Wasser, so wird zunächst vorteilhaft ein der Wassermenge entsprechender überschuß von Äthylendi.amin genommen, der beim Einengen und Trocknen wieder entfernt wird.The products dissolve easily in water, but little in alcohol. By They are broken down by alkalis and acids, even through carbonic acid. The solid products are crystalline with no fixed melting point. During melting and before melting they split off amine. Assuming the components in the presence of water, an excess of ethylenediamine corresponding to the amount of water is initially advantageous taken, which is removed again during concentration and drying.
Geht man von festem primärem Th.eophylli.näthyl.endi.amin ;aus, so braucht kein überschu,C von Diamin verwendet zu «erden. Beispiel 2o bis 4o Teile C, C-Phenyläthylbarbitttrsäur.e werden mit Zoo Teilen Theophyllm und 6oo Teilen Wasser angerührt. Unter' Rühren gibt man etwa 8o Teile Äthylendianv,n -unter Kühlen hinzu, bis Lösetag erfolgt ist. Dann wird im Vakuum zur Trockene eingedampft. Die Herstellung kann bei gutem Digerieren auch ohne Zusatz von Wasser durchgeführt werden, wobei sich die Masse erhitzt. Man kühlt rasch ab und trocknet im Vakuum.Assuming solid primary th.eophylli.näthyl.enediamine; from, so does not need to use an excess of diamine to ground. Example 2o to 4o parts C, C-Phenyläthylbarbitttrsäur.e are zoo parts Theophyllm and 600 parts Touched water. About 80 parts of ethylene glycol are added with stirring, while cooling added until the release day has occurred. It is then evaporated to dryness in vacuo. the If digestion is good, production can also be carried out without the addition of water, whereby the mass heats up. It is cooled rapidly and dried in vacuo.
Claims (1)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DEG84101D DE674241C (en) | 1931-07-31 | 1931-07-31 | Process for the preparation of readily soluble theophylline compounds |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DEG84101D DE674241C (en) | 1931-07-31 | 1931-07-31 | Process for the preparation of readily soluble theophylline compounds |
Publications (1)
Publication Number | Publication Date |
---|---|
DE674241C true DE674241C (en) | 1939-04-13 |
Family
ID=7137922
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DEG84101D Expired DE674241C (en) | 1931-07-31 | 1931-07-31 | Process for the preparation of readily soluble theophylline compounds |
Country Status (1)
Country | Link |
---|---|
DE (1) | DE674241C (en) |
-
1931
- 1931-07-31 DE DEG84101D patent/DE674241C/en not_active Expired
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