Industrial Hydrolases and Related Enzymes

Biocatalyzed synthesis of antidiabetic drugs: A review

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“…Although this process was scaled to grams, AZD 4619 was discontinued because of hepatotoxicity problems detected in Phase I (Thulin et al 2008). Similarly, the resolution of the racaemic alphachloro thioester intermediate 7 has been described using the same strategy, shown in Figure 8 (Dow et al 2012). Remarkably, the use of a protease instead of a lipase allowed the synthesis of the antipode (R)-8, although with a lower ee (90% with Savinase versus 98% with lipase).…”