Lewis acid-mediated Suzuki–Miyaura Cross-Coupling Reaction
Malvern Panalytical Pharmaceuticals
Supporting you in each stage of discovery, development and manufacture of (bio)pharmaceuticals.
A recent publication in ChemRxiv describing the use of Lewis acids to catalyse Suzuki reactions caught the attention of the members of our weekly journal club:
The well-established set up of a Suzuki reaction requires a base to couple an aryl halide and a boronic acid as it plays a crucial role in the catalytic cycle by facilitating the transmetallation. However, the use of the base limits the scope of the reaction as it can lead to undesired side reactions reducing product yield.
In this communication, a Zn-TMEDA complex, in place of a base allowed coupling of an aryl bromide and borate salt in good yield. The scope of the reaction was investigated and found to have an enhanced functional group tolerance and could also couple sterically hindered substrates.
This novel procedure is a promising application for late-stage functionalisation of bioactive compounds. At CLS/MP, we are involved in a multitude of challenging organic chemistry projects and the Suzuki reaction is routinely employed to access complex targets. We are excited to further test the scope of the reaction and improve upon our current synthetic procedures.?
Led by CLS research leader, Jamie Stokes, journal club provides an opportunity for our chemists to develop their knowledge and stay up-to-date with the latest research.
Communication specialist for hydrogen dissemination| Digital Content Creator & Science Communicator. I specialise in Organic Chemistry and Catalysis
2 年Thanks for publishing my article written in collaboration with Dr Jamie Stokes