50840-93-2Relevant academic research and scientific papers
Cyanoalkylamino-amido benzophenones
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, (2008/06/13)
The present invention relates to pharmacologically valuable new benzophenone derivatives having a pronounced sedative action on the central nervous system and some of which also possess muscle-relaxing and aggression-inhibiting properties. These new derivatives have the structural formula SPC1 And their addition salts, in which R1 and R2 are substituents selected from the group consisting of hydrogen, alkyl having 1-5 carbon atoms, alkenyl having 2 to 4 carbon atoms, alkinyl having 2 to 4 carbon atoms or β-bromoallyl (--CH2 --CBr = CH2) ; R3 is --CN; n is an integer selected from 1 and 2; and m is an integer selected from 1, 2 and 3, wherein the rings A and B may be substituted, ring A being substituted preferably with a halogen such as chlorine or with nitro, trifluoromethyl, methyl, methoxy or methylmercapto, preferably in the 5 position, and ring B being preferably substituted in the 2' position with chlorine or fluorine. The radical R1 preferably signify hydrogen or a methyl, ethyl or propargyl group, the radicals for R2 preferably signify hydrogen or a methyl, allyl or an n-butyl group. C compounds represented by the above structural formula may be produced by reacting a compound represented by the formula SPC2 With a compound having the formula Y -- Cm H2m -- R3, one of X and Y signifying the substituent R2 -- NH -- and the other signifying a halogen atom, preferably a bromine or chlorine atom, so as to form the above specified benzophenone derivative with the elimination of H -- Hal, R1, R2, R3, n and m being as defined above, and the rings A and B being optionally substituted as discussed above. The hydrogen halide which is eliminated is advantageously bound by the addition of an acid-binding agent, as for example, a molar excess of the amine used in the reaction or, for example, triethylamine, dimethylaniline, potassium or sodium carbonate or sodium bicarbonate. The reaction is carried out in a suitable solvent, preferably at an elevated temperature, typically the reflux temperature of the solvent used.
Benzophenone derivatives and process for their production II
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, (2013/12/13)
The present invention relates to a pharmacologically valuable new benzophenone derivatives having a pronounced sedative action on the central nervous system and some of which also possess muscle-relaxing and aggression-inhibiting properties. These new derivatives have the structural formula EQU1 and their acid addition salts, in which R 1 and R 2 are substituents selected from the group consisting of hydrogen, saturated and unsaturated alkyl groups having 1-4 carbon atoms; R 3 is a substituent selected from the group consisting of --CN, --CONH 2, --COOCH 3, --COOC 2 H 5, --COOH, and --COOMe, where Me is a metallic cation; n is an integer selected from 1 and 2; and m is an integer selected from 1,2, and 3, and wherein the rings A and B may be substituted, ring A being substituted preferably with a halogen such as chlorine or with nitro, trifluoromethyl, methyl, methoxy or methylmercapto, preferably in the 5 position, and ring B being preferably substituted in the 2'' position with chlorine or fluorine. The radicals R 1 and R 2 preferably signify hydrogen or a methyl group, or a n-butyl group in the case of Ring B.The metal cation Me is preferably a pharmacologically acceptable metal cation, as for example sodium, potassium, calcium or ammonium.Compounds represented by the above structural formula may be produced by reacting a compound represented by the formula EQU2 with a compound having the formula Y -- C m H 2m -- R 3, one of X and Y signifying the substituent R 2 -- NH -- and the other signifying a halogen atom, preferably a bromine or chlorine atom, so as to form the above specified benzophenone derivative with the elimination of H -- Hal, R 1, R 2, R 3, n and m being as defined above, and the rings A and B being optionally substituted as discussed above. The hydrogen halide which is eliminated is advantageously bound by the addition of an acid-binding agent, as for example, a molar excess of the amine used in the reaction or, for example, triethylamine, dimethylaniline, potassium or sodium carbonate or sodium bicarbonate. The reaction is carried out in a suitable solvent, preferably at an elevated temperature, typically the reflux temperature of the solvent used.
