Radical chemistry has received little attention in medicinal chemistry due to the fact that most reactions use organotin derivatives under high dilution conditions producing low amounts of product. Our research is based on the development of novel non-toxic tuneable methodology towards biologically active heterocycles, as shown below (Scheme 1). Scheme 1 We have successfully demonstrated that our non-toxic thiyl radical/isocyanide approach can produce diverse structures for various disease targets. Using this approach, we have been able to synthesize a large number of biologically active compounds, as shown (Table 1).Table 1 Imiquimod is used for treating various cancers such as skin and melanomas. It has recently attracted attention due to its neuroinflammatory modulation on several demyelinating diseases, including multiple sclerosis (MS). Our compounds being analogues to imiquimod they could be potential therapeutic candidates. Therefore the next stage of our research will focus on their effects on multiple sclerosis and our synthetic approach to these diverse classes will be described.

Tuneable radical cyclisations: Synthesis of biologically active heterocycles to target neuroinflammation

246th National Meeting (2013)

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