67499-62-1Relevant academic research and scientific papers
TOLPERISONE ANALOGS AND METHODS OF USE
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Page/Page column 29-31, (2019/10/29)
The present invention is, in part, directed to tolperisone analogs (e.g., compounds of formula (I), (I-a), (I-b), (II), (Il-a), (III), (Ill-a), (ΙΙΙ-b), (III-c), (IV), (IV-a), (V), or (V-a)) and methods of use thereof for the treatment of various conditions including elevated muscle tone and tension (e.g., spasticity, muscle spasm). In one aspect, the tolperisone analogs disclosed herein have an additional substituent at the α-position, which blocks the generation of a β- elimination product.
METHOD FOR PRODUCING SALTS OF TOLPERISONE
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Page/Page column 6-9, (2008/06/13)
The invention relates to a method for producing an addition salt of 2,4'-dimethyl-3-piperidino-propiophenone (tolperisone) with a pharmaceutically acceptable acid, of formula (I). According to the invention, 4-methylpropiophenone is reacted with piperidine hydrochloride and 1,2-dioxolane in the presence of an acid serving as a catalyst, and the tolperisone obtained in the form of an acid addition salt is separated by filtering after the reaction mixture has cooled down.
Synthesis of 3H-tolperisone
Dietrich, Axel,Fels, Gregor
, p. 1125 - 1134 (2007/10/03)
Tolperisone has been tritiated to 50 Ci/mmol specific activity in order to use this compound in the study of muscle relaxant binding. Of the two reaction pathways investigated, hydrogenolytic exchange of aromatic bromine is favored over hydrogenation of a double bond.
A modified Mannich reaction using 1,3-dioxolane
Sumita,Koumori,Ohno
, p. 1676 - 1678 (2007/10/02)
Mannich reaction of ketones using 1,3-dioxolane instead of formaldehyde, paraformaldehyde, or 1,3,5-trioxane afforded the corresponding Mannich bases in high yields. Under the same conditions the aminomethylation of aromatics did not proceed but the intramolecular aminomethylation, like a Pictet-Spengler type reaction, proceeded smoothly.
Process for the preparation of tertiary amines
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, (2008/06/13)
Certain tertiary amines useful as pharmaceuticals are prepared in improved yields by condensing a cyclic secondary amine with a primary alkyl halide in an aqueous medium in the presence of an acid acceptor.
