Light mediated synthesis and functionalization of N-heterocycles

N-heterocycles are ubiquitous in medicinal drugs with over 60% of small molecule drugs containing them However, available chemical strategies to synthesise and functionalise these rings are limited This restricts the structures accessible and the chemical space available to scientists.

Currently the majority of rings are 5 or 6 membered with only ~4% being medium sized 7 or 8 membered rings. This is due to reduced thermodynamic stability compared to their parent 5 or 6 membered rings. Because of this, access to this structure is difficult and often require chemical reactions which use expensive and toxic transition metals, that presents issues of sustainability.

One reason to functionalise these drugs is for structure activity relations showing which areas of functionalisation improve the effectiveness of said drug. However, under the current methods a new synthetic pathway is needed, or changes to the pathway early on are required for these drug libraries to be made. Late-stage functionalisation can be used to solve this in altering the drugs at the end of the pathway, meaning a bulk sample of the drug can be made then a few reactions can be done to modify the drug for the SAR studies.