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Optimized synthesis and solid state investigations on the drug candidate encenicline hydrochloride
For the production of drug substances a robust, scalable process delivering the active pharmaceutical ingredient (API) in excellent chemical and polymorphic purity is required. For this purpose we developed a novel imidazole-mediated one-pot procedure for the preparation of encenicline hydrochloride monohydrate, which crystallizes directly from the reaction mixture as pure non-hygroscopic polymorph (Form I). Solid state studies revealed a series of additional new physical forms for which crystal structures have been determined by single crystal X-ray diffraction.
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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H149N | ChemSpider