A New Convergent Catalytic Synthesis of Azetidines

This collaboration will deliver a novel convergent method for the construction of medicinally-relevant azetidines. The project involves a [3+2] cycloaddition in combination with an unprecedented reductive cyclisation reaction of isoxazolidines recently discovered in our laboratory, that utilises a silane and metal catalyst. The new chemistry will be developed for the synthesis of drug discovery building blocks as well as a late-stage azetidinylation process. This cycloaddition/ reductive cyclisation could then be applied to analogous substrates such as 3,6-dihydro-2H-1,2-oxazines to make the 3-pyrroline products.