Making Complex Chiral Amines by Catalytic Resolution-Racemisation-Recycle (R3-Process)

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This project aims to build-upon and move rapidly to exploit an exciting new process to make optically active amines that started with a current AZ supported CASE studentship (Blacker/Munday/Kwan). The method takes advantage of the benefits of diastereomeric crystal resolution - high selectivity, simple robust and scalable process, low cost and widely applicable, and overcomes the major limitation - maximum 50% yield with associated waste and cost issues. Thus far the scope has been evaluated with a series of 2o and 3o chiral amines, typically made in >80% yield and >95% e.e. We now wish to widen the scope of the R3-Process by researching optically active b-amino alcohols, and related chiral centres, that are frequently encountered in development compounds. A further aspect is to develop an understanding of diastereomer solubility to assist in solvent selection and predict salt pairs. The project addresses the AZ PhD Collaborations Call in developing a new more efficient method of product isolation.