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Dr. Tomas Hudlicky

Canada Research Chair

Brock University, Ontario

Chemoenzymatic total synthesis of natural products: recent progress in approaches to morphine and other complex targets

Abstract: The lecture will provide a brief introduction to biocatalytic methods in synthesis. Specifically, the use of various aromatic dioxygenase enzymes will be highlighted and their applications in total synthesis will be presented. These include several total syntheses of morphine alkaloids, total synthesis of Amaryllidaceae alkaloids and their medicinally useful derivatives, and approaches to other, highly oxygenated compounds such as xylosmin, tetrodotoxin, and idesolide. Biological activities will be included where relevant. Highlights of our process development for the industrial production of opiate-derived medicinal agents will also be presented with a discussion of academic versus industrial requirements for solutions to problems. A short discussion of efficiency metrics will be provided at the conclusion of the lecture.



Dr. Michael Zaworotko Sponsored by ACENET

Bernal Chair of Crystal Engineering 

University of Limerick, Limerick, Ireland

Crystal Engineering: Form to Function

Abstract:That composition and structure profoundly impact the properties of crystalline solids has provided impetus for exponential growth in the field of crystal engineering1 over the past 25 years. This lecture will address how crystal engineering has evolved from structure design (form) to control over bulk properties (function). Strategies for the generation of two classes of functional crystalline materials will be addressed:



Multicomponent pharmaceutical materials, MPMs, such as cocrystals2 have emerged at the preformulation stage of drug development. This results from their modular and designable nature which facilitates the discovery of new crystal forms of active pharmaceutical ingredients, APIs, with changed physicochemical properties. The concepts of “supramolecular heterosynthons” and “ionic cocrystals” will be explained and a case study addressing brain bioavailability of lithium will be presented.



Hybrid Ultramicroporous Materials, HUMs, are built from metal or metal cluster “nodes” and combinations of organic and inorganic “linkers”. Two families of HUMs that afford exceptional control over pore chemistry, pore size and binding energy, will be detailed. Benchmark selectivity for CO2 capture in these HUMs with pcu or mmo (see Figure) topology has been observed3 thanks to the strong electrostatics associated with pores lined by the inorganic components of these nets. Interpenetrated 3D nets, another understudied class of material, also afford control over pore size and will also be addressed.

 In summary, this lecture will emphasize how crystal engineering coupled with molecular modeling can offer a paradigm shift from the more random, high-throughput methods that have traditionally been utilized in materials discovery and development. In short, crystal engineering can teach us how to custom-design the right material for the right application.

References

1. (a) Desiraju, G.R. Crystal engineering: The design of organic solids Elsevier, 1989; (b) Moulton, B.; Zaworotko, M.J. Chemical Reviews 2001, 101, 1629-1658.

2. Duggirala, N.; Perry, M.L.; Almarsson, Ö.; Zaworotko, M.J. Chem. Commun. 52, 640-655, 2016.

3. Nugent, P.; Belmabkhout, Y.; Burd, S.D.; Cairns, A.J.; Luebke, R.; Forrest, K.; Pham, T.; Ma, S.; Space, B.; Wojtas, L.; Eddaoudi, M.; Zaworotko, M.J. Nature 2013, 495, 80-84, 2013.