TH3293B - Process for the preparation of derivatives of 5H-2,3-benzodiazepines And pharmaceutical mixtures containing these substances - Google Patents

Abstract

This invention deals with the process of preparing 5H-2,3-benzodiazepines of the general formula (I) and the salts resulting from these compounds with pharmacologically acceptable acids (chemical formulas), where R and R1 each represent hydrogen, chlorine. , C1-4 alkyl or C1-4 alkyl, R2 instead of hydrogen, or C1-4 alkyl, R3 and R4 each representing C1-4 alkyl when combined in place of methylene. new derivative of 1-Aryl-5H-2,3-benzodiazepine of this invention has beneficial effects on the central nervous system, especially against aggression, anxiety, drowsiness and inducing sleep. Pharmacy of this invention There are compounds of formula (I) or salts formed from these compounds with pharmacologically acceptable acids. At least one of them is an active ingredient that can be used as a useful medicinal drug.

Claims (7)

1. The process for the preparation of 5H-2, 3-benzodiazepines of the general formula (I) and salts formed from these compounds combine with pharmacologically acceptable acids (chemical formulas), where R and R1 each Hydrogen, Chlorine, C1-4 Alkyl Agent or C1-4 Lkyl, R2 Hydrogen or C1-4 Alkyl R3 and R4 Each C1-4 Alkyl Agent When combined instead of methylene. A Characterized by the general formula (II) compound reduse (chemical formula), which R, R1, R2, R3 and R4 have the meanings defined above, in organic solvents and, if desired, change the resulting compound. Of the general formula (I) to form a salt formed by acidification, which is acceptable in medicine, or to prepare the free base of the general formula (I) from its salts and convert to acidic salts. Another kind 2. The process of claim 1, which is characterized by the compound of the general formula (II), catalyzes hydrogenation. 3. The process of claim No. 1, which is unique as follows: Also reacts reductive Hydrazine or hydrazine hydrate, with a catalyst 4. Procedures of Claims 1 to 3, one of which is characterized by using palladium, platinum or raynickel. Is a catalist 5. Procedures of Clause 1 to 4, one of which is unique: C1-4 alcohol, dioxane, tetrahydrofuran, benzene, toluene, xylene. , Dimethyl formate, dimethyl acetate, or a mixture of these substances as solvents. 6. Process of any 1 to 5 claim. Which has the characteristics Perform a reductive reaction at a temperature between room temperature and the boiling point of the solvent. 7. Process for preparing pharmaceutical mixtures Which acts on the central nervous system Which has the characteristics Change the general formula (I) compound prepared by the sole method of claiming in claim 1. Or mixed with other compounds that produce similar results But no synergistic effect on generic formulas (I), if desired, mix fillers, carriers, surfactants, flavoring agents, in the form of tablets, capsules, tablets, suppositories, emulsions, Suspensions, injection solutions, etc. by clinically known methods