Abstract
The convenient oxidation was carried out to Rimonabant and its analogue with mCPBA for the formation of their reactive biological metabolites. The lactam oxidized Rimonabant metabolite was first successfully synthesized for demonstrating the construction and characterized by NMR spectroscopic methods and the single-crystal X-ray diffraction study. Through metabolism study of Rimonabant in vivo in mice, the lactam metabolite belongs to one of many high levels of reactive oxidized Rimonabant metabolites. On the other hand, the lactam metabolite is the most stable form in snapshot PK test and displays markedly reduced brain penetrance.
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