The Hantzsch reaction is known for more than 100 years. Medicinal chemists have used this reaction to gain easy access to very important heterocyclic scaffolds such as 1,4-Dihydropyridines and Pyrroles. 1,4-Dihydropyridine molecules have shown to be potent blockers of calcium channels as well as activators of potassium channels. The specific activities are reflected by different substitution patterns. We have developed a two-step synthesis towards Naphthyridines and Aza-Indoles. Our strategy relies on treating the appropriate Hantsczh reaction product with N-Bromosuccinimide in DMF at ambient temperature. The scope of this novel oxidation reaction has been studied and will be disclosed.

Efficient synthesis of drug-like polycyclic compounds such as naphthyridines and aza-indoles

251st National Meeting (2016)

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