Pharmaceutical chiral

Biocatalysis has emerged as an important tool for the enantioselective synthesis of chiral pharmaceutical intermediates and several review articles have been published in recent years [133-137]. For example, quinuclidinol is a common pharmacophore of neuromodulators acting on muscarinic receptors (Figure 6.50). (JJ)-Quinudidin-3-ol was prepared via Aspergillus melleus protease-mediated enantioselective hydrolysis of the racemic butyrate [54,138]. Calcium hydroxide served as a scavenger of butyric acid to prevent enzyme inhibition and the unwanted (R) enantiomer was racemized over Raney Co under hydrogen for recycling. 

Gotor-Fernandez, V., ReboDedo, F. and Gotor, V. (2007) Preparation of chiral pharmaceuticals through enzymatic acylation of alcohols and amines, in Biocatalysis in the Pharmaceutical and Biotechnology Industry, (ed. R.M. Patel), Dekker, Taylor and Francis, New York, Chapter 7, pp. 203-248. 

The growth of industrial scale biotransformation processes has increased significantly over recent years with more than 130 reported in 2002 [1]. Major activity is focussed on the production of chiral pharmaceuticals although a number of large scale industrial processes have been developed for the food and agricultural industries. 

Lubda, D., Cabrera, K., Nakanishi, K., Lindner, W. (2003). Monolithic silica columns with chemically bonded b-cyclodextrin as a stationary phase for enantiomer separations of chiral pharmaceuticals. Anal. Bioanal. Chem. 377, 892-901. 

Bommarius, A.S., Scharm, M. and Drauz, K. (1998) Biocatalysis to amino acid-based chiral pharmaceuticals -examples and perspectives. Journal of Molecular Catalysis B, Enzymatic, 5, 1-11. 

Ager, D.J., Li, T., Pantaleone, D.P. et al. (2001) Novel biosynthetic routes to non-proteinogenic amino acids as chiral pharmaceutical intermediates. Journal of Molecular Catalysis B, Enzymatic, 11 (4—6), 199-205. 

Application of Whole-Cell Biotransformation Process in the Synthesis of Chiral Pharmaceutical Intermediates... 

Patel, R.N. (2007) Biocatalysis for synthesis for chiral pharmaceutical intermediates, in Biocatalysis in the Pharmaceutical and Biotechnology Industries (ed. R.N. Patel), CRC Press, Boca Raton, FL, pp. 103-158. 

Buser, H.-R., Poiger, T. and Muller, M. D. (1999). Occurrence and environmental behaviour of the chiral pharmaceutical ibuprofen in surface waters and in waste-water, Environ. Sci. Technol., 33, 2529-2535. 

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