Strategies for the Diversity-Oriented Synthesis of Macrocycles.

It is interesting how these things happen. Last week, we held GalChimia Day, an initiative to share the knowledge and experience of experts from the pharmaceutical and biotech industry in the field of drug discovery and development with our clients and the scientific community. The first edition was entitled ‘Challenges in Drug Discovery’, and Enrique Fernández, a Project Manager in our labs at the PCB, presented ‘Macrocycles in the Pharmaceutical Industry’. His presentation focused on the big opportunity that macrocycles offer to explore an area of the chemical space that can provide valuable compounds against targets that are hardly accessible through common small molecules. A week ago, the FDA approved Vyleesi (bremelanotide), which is a cyclic heptapeptide lactam analogue of the a-melanocyte-stimulating hormone (a-MSH).

And now, this. It is a review by Spring et al. (University of Cambridge, UK) covering strategies for the Diversity-Oriented Synthesis of Macrocycles. That is, not tactics (i.e., reactions) for the cyclization, but new ways to design the synthesis of entire libraries of macrocycles. If you are not familiar with Diversity-Oriented Synthesis (aka DOS, not to be confused with the old operating system), check the original work by Stuart L. Schreiber in Nature.


Strategies for the Diversity-Oriented Synthesis of Macrocycles
Chem. Rev. 2019, Article ASAP.
See: 10.1021/acs.chemrev.9b00084