Functionalized azaheterocycles are found in many pharmaceuticals, making them extremely attractive to the synthesis and medicinal communities alike. The research applied a method for the cost-effective, rapid, and modular synthesis of azaheterocycle derivatives from 1,3-azadienes and 6-membered cyclic anhydrides. The synthesized products were successfully carried forward into a multitude of relevant reactions including the formation of tertiary alcohols, epoxidation reactions, and enol etherification. The approach to synthesis of these azaheterocycles has many advantages, such as a broad scope, high yields, cost-effectiveness, and simple protocols that are promising to drug discovery programs. Additionally, selected azaheterocycles from the assembled library are currently undergoing biological testing to determine the potential for cytotoxicity in humans and identify useful pharmacological effects against <i>Leishmania major</i> infection.

Synthesis, chemical reactivity, and medicinal activity of novel chiral piperidines

253rd National Meeting (2017)

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