PROCEDURE FOR THE PRODUCTION OF NEW AMINOALKYL HETEROCYCLEN AND YOUR SAEUREADDITIONSSALZEN

The invention concerns a procedure for the production of new Aminoalkylheterocyclen of the general formula R3 OH in the Q one the best one or I (lla) (IIb) IO represents, where R and R2, which can be also alike, hydrogen, halogen, tri fluorine methyl or Methoxy, A a bivalent remainder of NH, NCH3, OCH2 (whereby the oxygen is bound to the benzene ring) or - CH: - CH: - mean, n for a whole number from 2 to 6, RA a NH-Acetyloder the NH-CCNH: - Remainder means and R and R s, which can be also alike, for hydrogen, Hydroxymethyl, methyl, Methoxy, Nitro, Nitrilo, CONH2, Benzyloxy, together also for one the bivalent Reste-O-CH2 - o, - CH=CH-CH=CH, - O-CH2 - CO-NH, - CH2 - CH: - CO-NHoder - O-CO-NHstehen, if necessary in the form of Racematen or individual optical antipodes, and their acid addition salts. The procedure according to invention is characterized by that one tt a connection of the general formula Q-CnH2n-CnH2n2-CHOH NH2 4 - x (III) where Q, n, R and R-S the above meaning have and Xein represents anion, with Aoetanhydrid and/or Cyanat and acid convert, whereby the aliphatic bound amino group by addition of additionally at least 1 Moi acid per mol of the connection (III), and gewünschtenfalls a received Racemat of the general formula (I) into the optical antipodes is protected and/or a received connection of the general formula (I) isolates transferred into an acid addition salt. The basic materials for the procedure according to invention are received according to well-known methods. Producible the according to invention connections are valuable medicine materials and intermediate products, in particular for the synthesis of medicine materials. To emphasize is the container-extending effect, which permits also the use of the substances as Antihypertonika, Broncholytika and blood circulation-promoting means. Related connections 6ind already described into at-PS Nr.253499 and 258282. With the connections mentioned there it concerns however such, which gemäht at the nitrogen in contrast to the invention producible connections not a Phenyläthanol, but a Aralkylgruppe contained. The before-descriptive connections were suggested, differently as producible the according to invention connections, than tranquilizers and/or Tranquilizer. For application producible the according to invention new active substances with the auxiliary materials usual in galenischen pharmacy are converted to common drug forms, z • B • to tablets, dragee it, caps, Tinkturen, injection solutions. Suppositorien, inhalation preparations. I0 the single dose amounts to between 1 and 500 mg, preferably 2 to 200 mg; as a function of application form, active substance and body weight of the person who can be treated. The high dosages are possible particularly for Retardformen. Below examples of drug preparations are indicated. Tablets composition: Active substance manufactured in accordance with the invention 2 Gew. - Parts of stearic acid 6 Gew. - Parts grape sugar 5 9 2 Gew. - Parts the components are processed in usual way to tablets by 600 mg weight. Wishing case can be increased the active substance content or decreased and the grape sugar quantity decreased accordingly or increased. Suppositorien composition: Active substance manufactured in accordance with the invention 100 Gew. - Parts of Laktose, powdered 45 Gew. - Parts of cocoa butter 1 S 5 5 Gew. - Parts the components are processed in usual way to Suppositorien by 1,7 g weight. Caps composition: Active substance manufactured in accordance with the invention Laktose corn strength Gew. - Parts of 4 9 0 Gew. - Parts of 400 Gew. - Parts ever 1000 of mg of the finely pulverized mixture filled up in hard gelatin capsules • example 1: NHGOCH s, CH-CH, - NH-C (OH,), - N/ --'H a mixture of 3,9 g NB, I OH CH, I • HCI and 2 g acetic anhydrid in 40 ml dimethylformamide is warmed up I h on the cooking Wasserbad. After the Abdesti [lieren the solvent under vacuum the base with ammonia one sets free, to ethyl acetates one takes up and one dries. The ethyl acetate is abdestilliert and the base is shifted in acetonitrile with the computed quantity of maleic acid. The verse connection designated above is received as Maleinat in a yield from 3,5 g. The stop. after recrystallizing from methanol is 202°C. Example 2: NHCONH 2 CHa I CH-CH2-NH-C (CH2) - N “I I où 2” Nf V a solution of 6,1 g I0 NH2 CH3 I -- , - NH-C " (CH 2) OH 0 • HCI in a mixture of 20 ml water and 7.5 ml glacial acetic acid is shifted with a solution from 1,41 g Kaliumeyanat in 7,5 ml water with 35°C. After standing over night the base with ammonia is set free, separated by threefold Ausschütteln with ISO butanol and transferred in methanol into the Maleinat. 6 g are received from the connection designated above as Maleinat, those after recrystallizing from water the stop. 202°C show.