Integrated Biocatalysis in Multistep Drug Synthesis without Intermediate Isolation: A de Novo Approach toward a Rosuvastatin Key Building Block

Metzner R, Hummel W, Wetterich F, Koenig B, Gröger H (2015)
Organic Process Research & Development 19(6): 635-638.

Journal Article | Published | English

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In this contribution, we report the chemoenzymatic preparation of a key building block for the active pharmaceutical ingredient rosuvastatin, one of the "top 5 blockbuster drugs" with a worldwide market value of 6.25 billion USD in 2012, via a seven-step synthesis without isolation of intermediates and with incorporation of two highly efficient biotransformations. This chemoenzymatic process reaches excellent space-time yields by using high substrate concentrations (several hundred grams per liter), emphasizing the potential of biocatalysis for industrial processes related to pharmaceutical drug synthesis and the compatibility of enzyme chemistry with classical organic synthesis.
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Metzner R, Hummel W, Wetterich F, Koenig B, Gröger H. Integrated Biocatalysis in Multistep Drug Synthesis without Intermediate Isolation: A de Novo Approach toward a Rosuvastatin Key Building Block. Organic Process Research & Development. 2015;19(6):635-638.
Metzner, R., Hummel, W., Wetterich, F., Koenig, B., & Gröger, H. (2015). Integrated Biocatalysis in Multistep Drug Synthesis without Intermediate Isolation: A de Novo Approach toward a Rosuvastatin Key Building Block. Organic Process Research & Development, 19(6), 635-638.
Metzner, R., Hummel, W., Wetterich, F., Koenig, B., and Gröger, H. (2015). Integrated Biocatalysis in Multistep Drug Synthesis without Intermediate Isolation: A de Novo Approach toward a Rosuvastatin Key Building Block. Organic Process Research & Development 19, 635-638.
Metzner, R., et al., 2015. Integrated Biocatalysis in Multistep Drug Synthesis without Intermediate Isolation: A de Novo Approach toward a Rosuvastatin Key Building Block. Organic Process Research & Development, 19(6), p 635-638.
R. Metzner, et al., “Integrated Biocatalysis in Multistep Drug Synthesis without Intermediate Isolation: A de Novo Approach toward a Rosuvastatin Key Building Block”, Organic Process Research & Development, vol. 19, 2015, pp. 635-638.
Metzner, R., Hummel, W., Wetterich, F., Koenig, B., Gröger, H.: Integrated Biocatalysis in Multistep Drug Synthesis without Intermediate Isolation: A de Novo Approach toward a Rosuvastatin Key Building Block. Organic Process Research & Development. 19, 635-638 (2015).
Metzner, Richard, Hummel, Werner, Wetterich, Frank, Koenig, Burghard, and Gröger, Harald. “Integrated Biocatalysis in Multistep Drug Synthesis without Intermediate Isolation: A de Novo Approach toward a Rosuvastatin Key Building Block”. Organic Process Research & Development 19.6 (2015): 635-638.
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