Exploring Catalysis in API Synthesis - Pharmaceutical Technology

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Exploring Catalysis in API Synthesis
Chemocatalysis and biocatalysis are important elements of an effective strategy for improving yield and stereoselectivty.

Pharmaceutical Technology
Volume 34, Issue 5, pp. 42-46

Systems catalysis

The NRSC-Catalysis program is also advancing a systems approach to catalysis, which analyzes functional catalytic systems in which multiple molecular processes are combined and regulated to carry out a catalytic operation. The goal of systems catalysis is to combine homogeneous, heterogeneous, and biocatalytic methods. A potential advantage of a systems approach to catalysis is to create "one-pot" multiple component catalyst systems for multistep synthesis. Most traditional synthesis is performed sequentially by ending one reaction step and then proceeding to the next reaction step, which may involve solvent and temperature swaps, liquid–liquid extractions, product crystallization, chromatographic purification, distillation, the addition or removal of protecting groups, and the addition and removal of reagents and catalysts. A systems approach would allow for a more directed way of developing catalytic reaction sequences and one-pot multicomponent catalyst systems (5).

Asymmetric synthesis

Strategies in asymmetric synthesis is an area of ongoing interest, particularly in the production of pharmaceutical compounds. In 2009, researchers from the University of Bristol in the United Kingdom and the University of Gothenburg in Sweden reported findings from their work in palladium-based asymmetric catalysis. The key finding was structural and mechanistic information on Trost modular ligands (TMLs), which combine with palladium to form catalysts. TML-Pd catalysts are widely used in allylic substitution reactions (8, 9). Their new model involved two regiochemically distinct (NH) and (CO) locations for nucleofuge or nucleophile binding, which may have broad utility for understanding the selectivity in asymmetric allylic alkylation reactions catalyzed by select palladium complexes and related ligands (8, 9).

Patricia Van Arnum is a senior editor at Pharmaceutical Technology, 485 Route One South, Bldg F, First Floor, Iselin, NJ 08830 tel. 732.346.3072,


1. J. Wassenaar et al., Nat. Chem. 2 (5), 417–421 (2010).

2. S. Borman, Chem. & Eng. News 88 (14), 7 (2010).

3. S. Ritter, N. Becker, and T. Blair, Chem. & Eng. News 87 (51), 35–39 (2009).

4. S.L. Desset and D.J. Cole-Hamilton, Angew. Chem., Int. Ed. Engl. 48 (8), 1472–1474 (2009).

5. NRSC-Catalysis, Future Perspectives in Catalysis (Amsterdam), http://www.nrsc-catalysis.nl/files/media/scientific_reports/Future_perspectives_in_Catalysis.pdf, accessed Apr. 5, 2010.

6. D. Toste et al., Nat. Chem. 2 (1), 36–41 (2010).

7. M. Jacoby, Chem. & Eng. News 87 (49), 10 (2009).

8. S. Borman, Chem. & Eng. News 87 (24), 31–33 (2009).

9. G.C. Lloyd. J. Am. Chem. Soc ., 131 (8), 9945–9957 (2009).


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