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PROCESS FOR THE PREPARATION OF CENOBAMATE
P202230648
The invention relates to a novel process for the synthesis of 1-(2-chlorophenyl)-2-(2H-tetrazol-2-yl) ethyl carbamate, the active ingredient of the drug cenobamate, marketed as Ontozry® in Europe and Xcopri® in USA. Said process can be carried out in steps or sequentially in a single reaction step, without the need to isolate the intermediates. The process is characterized by the use of mechanochemistry as a source of energy in the synthetic process and by the regioselective production of nitrogen-substituted tetrazoles in position 2. The described process is fast, respectful with the environment and profitable from the economic point of view.
ADVANTAGES The invention describes a synthetic process that is performed regioselectively in one of its reaction steps, it which doubles the yields of the reaction. On the other hand, the times of reaction, does not use solvents, is a one-pot process that does not isolate intermediates in such a way that describes a highly profitable process from the environmental and economic point of view. The process is done by grinding, without the need for external heat input. APPLICATIONS The invention opens the possibility of developing a manufacturing process for the active pharmaceutical ingredient cenobamate or its synthetic intermediates, in a mechanochemical process with low environmental impact and high regioselection, the which can be done continuously by using extrusion screws.
Patent applied for with priority date 07/14/2022. Unpublished.