论文信息 - Multi-step continuous flow synthesis of fluconazole

Multi-step continuous flow synthesis of fluconazole

AbstractThe development of a flow chemistry approach to the anti-fungal fluconazole is described. A continuous, two-reactor, three-step synthesis of fluconazole from 2-chloro-2′,4′-difluoroacetophenone was achieved with no intermediate purification. The synthesis has been successfully demonstrated on a Vapourtec commercial flow chemistry system. Graphical abstractᅟ

[1] R. Becher,et al. Fungal cytochrome P450 sterol 14α-demethylase (CYP51) and azole resistance in plant and human pathogens , 2012, Applied Microbiology and Biotechnology.

[2] Perrer N. Tosso,et al. The Application of a Continuous Grignard Reaction in the Preparation of Fluconazole , 2017 .

[3] F. Abe,et al. Fluconazole modulates membrane rigidity, heterogeneity, and water penetration into the plasma membrane in Saccharomyces cerevisiae. , 2009, Biochemistry.