The invention discloses a deuterated lamiterone
medicine as well as a preparation method and application thereof, and relates to the technical field of lamiterone, the preparation method comprises the following steps: firstly weighing deuterated propionic acid, and then adding
dichloromethane, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide
hydrochloride and 1-
hydroxybenzotriazole to obtain white turbid liquid; dropwise adding the
mixed solution into the white turbid liquid, stirring and reacting overnight, adding water for
quenching, extracting twice by using
dichloromethane, washing by using a saturated
saline solution,
drying by using
anhydrous sodium sulfate, and concentrating to obtain a crude product; performing
column chromatography separation on the crude product, concentrating and
drying to obtain a deuterated lamiterone
medicine; according to the deuterated lamiterone
medicine as well as the preparation method and the application thereof,
hydrogen atoms at key positions in lamiterone molecules are replaced with
deuterium atoms, so that the
metabolic rate of deuterated lamiterone is reduced, the half-life period of deuterated lamiterone is prolonged, and the
sleep time of a patient is prolonged.