DE281009C - - Google Patents

Description

IMPERIAL

PATENT OFFICE.

PATENT LETTERING

CLASS 12 g. GROUP

There are already various known compounds that mercury on one side aromatic Contain bound cores and have preference over mercury salicylate, to deliver neutral soluble alkali salts. Such compounds are e.g. B. the mercury compounds of oxybenzoic sulfonic acids (cf. patent specification 216267, class 12 q). These bodies are partly already medically introduced,

z. B. the mercurisalicylsulfosaure sodium in a mixture with Acoin under the trade name Embarin.

It has now been found that mercury in particular has one side of the aromatic Arylsulfonic acids containing an amine group are medically effective contain.

The effect of organically bound mercury on the organism is closely related to the purely chemical separability of the mercury from the organic bond. As is well known, the behavior of organic mercury compounds towards sulfur ammonium provides a standard for this (see Bioehem. Zeitschr. Vol. 33, p. 398). While the toxic mercurianiline reacts immediately with ammonium sulphide, which means that the mercury releases immediately and is therefore too toxic to be used for injection purposes, the sodium mercury dibenzoic acid sodium Hg (C ₆ H ₄ COOH) ₂ only becomes after about three weeks with the excretion of mercury sulfide blackened. Because the mercury is difficult to split off, it is not effective enough and therefore has no therapeutic value. The sodium mercurisalicylsulfosaure shows blackening with sulfur ammonium after V ₂ to 1 hour. The embarin, the action of which is based on this salt, splits off the mercury fairly quickly, and therefore often has too violent an effect on patients who are sensitive to mercury. It is therapeutically very important abstufen the removability of mercury largely and can customize the _t individual case and the sensitivity of the individual patient. The present invention opens up a possibility for this. It has. it has been shown that the introduction of the amino group into the organic compounds to be combined with mercury permits a substantial gradation of the cleavage of the mercury compound; the sodium mercurimetanilsaure z. B. is only blackened by sulfur ammonium after about 24 hours and gives the opportunity to introduce mercury into the body in a milder, but sufficiently fast-acting form. On the other hand, the stability of the mercury in the aminoarylsulfonic acids can be influenced as required by a suitable choice of the substituents on the aromatic nucleus. Thus, by introducing the hydroxyl group into the aminobenzenesulfonic acid, the corresponding mercury compound can be cleaved much more easily than the non-hydroxylated compound.

The preparation of the new compounds takes place in such a way that one aminoarylsulfosaures Mercury or a mixture of amino

aryl sulfonic acids with their mercury salt-supplying substances are heated until the resulting aromatic mercury compound has become alkali-soluble.
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Example i.

Sodium mercurimetanilic acid.

20 g of metanilic acid are made from 15.5 g Mercury chloride freshly prepared mercury oxide stirred in an aqueous suspension, until all the oxide is gone. The aqueous suspension is warmed in a water bath for so long until there is no longer any separation of mercury oxide by sodium hydroxide solution. Man sucks lukewarm, wash with water and dissolve the filter residue by adding sodium hydroxide solution in a little water. The sodium salt, which is readily soluble in water, is obtained by introducing the solution in alcohol. It contains that Mercury in a solid organic bond, because ammonium sulphide is in the No mercury sulfide is split off when standing for several hours in the cold.

Instead of metanilic acid one can use other aminoarylsulfonic acids, z. B. ■ aminophenolsulfonic acids, aminobenzoesulfonic acids and similar acids use.

Example 2.

Mercuriaminophenolsulfosaures
Sodium.

30 g of aminophenolsulfonic acid III (Beilstein, II. Supplementary Volume, p. 492) are dissolved in water dissolved and stirred for some time with the freshly prepared mercury oxide from 20g of sublimate. The mass is then heated in the water bath until the color is initially yellowish colored precipitate has changed to white (caustic soda does not cause any Separation of mercury oxide, but a clear solution). You vacuum off, wash with Water and dissolves the residue in water by adding sodium hydroxide solution. By registering the solution in alcohol precipitates the sodium salt, which is readily soluble in water, with a white color.

Example 3.

Sodium acid salt of mercuri-m- - ₀ aminosulfobenzoic acid.

4.32 g of m-aminosulfobenzoic acid, prepared according to patent specification 109487 (Beilstein, supplementary volume II, p. 807), are converted into the acidic sodium salt and in dilute aqueous solution at about 35 ° with 1.99 g yellow mercury oxide until it has disappeared. One then heats until boiling until no mercury oxide is deposited in a sample by sodium hydroxide solution more takes place, but a clear solution occurs. The mercury oxide is then in that acidic sodium salt of mercury-m-aminosulfobenzoic acid, which is converted from the Reaction mixture is obtained as a brown powder by suction. The connection gives the usual mercury reactions only after boiling with hydrochloric acid.

Claims (1)

Patent claim: Process for the production of mercured aminoarylsulfonic acids, characterized in that that one forms aminoarylsulfonic acid mercury or mixtures of aminoarylsulfonic acids with their mercury salt Materials heated until the mercury compound formed is alkali-soluble has become.