Fantastic to see our scientists' contributions being showcased once more through publication.

Prioritising delivery and adding value to our clients’ drug development projects is paramount. Our seasoned process chemists recent work supported our client in developing a safe and scalable route to a key intermediate on multikilogram scale.

Access the full paper here:  Development of a Safe and Scalable Method to Prepare 3-Bromo-N-alkyl-1,6-naphthyridones via Enamine Cyclization | Organic Process Research & Development (acs.org)

Route scouting plays a critical step in drug development by identifying the most efficient and cost-effective pathways in making key intermediates and APIs. By evaluating several routes, we can mitigate risks, reduce development time and enhance the overall success rate when manufacturing on large scale.

N-alkyl-naphthyridones and naphthyridines are motifs utilised in several APIs.  Literature precedence to access this fragment flagged safety concerns; with toxic reagents / by-products being used /formed as well as sharp exotherm detected – clearly a route that is not scalable! Formation of a stable enamine intermediate was much more attractive way in to the naphthyridones. Moreover, this route offered versatility, as the relevant amine can be ‘dialled-in’ to form N-alkyl-naphthyridones without any concerns over N vs O alkylation.  

If you would like to tap into our expertise in designing scalable processes for manufacturing as well as our track record in delivering complex small molecule targets fill in our contact form today.

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