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The Process Development of Ravuconazole: An Efficient Multikilogram Scale Preparation of an Antifungal Agent

2009; American Chemical Society; Volume: 13; Issue: 4 Linguagem: Inglês

10.1021/op900065c

1520-586X

Jaan A. Pesti, Chien‐Kuang Chen, Lori A. Spangler, Albert J. DelMonte, Serge Benoit, Derek D. Berglund, Jeffrey T. Bien, Paul R. Brodfuehrer, Yeung Chan, Elisabeth Corbett, Carrie Costello, Paul Demena, Robert P. Discordia, Wendel W. Doubleday, Zhinong Gao, Stéphane Gingras, John A. Grosso, Oscar W. Haas, David J. Kacsur, Chiajen Lai, Simon Leung, Melanie M. Miller, Jale Müslehiddinoğlu, Nina Nguyen, Jun Qiu, Martina Olzog, Emily Reiff, D. Thoraval, Michael J. Totleben, Dale Vanyo, Purushotham Vemishetti, John Wasylak, Chenkou Wei,

Antifungal resistance and susceptibility

The development of a safe, robust process for the preparation of ravuconazole (1), an antifungal agent, is described. The discovery and development of procedures enabling the efficient synthesis of multikilogram quantities of 1 and the process demonstration through plant scale preparations are presented. A controlled means to prepare a Grignard reagent and utilization of Fourier Transform Infrared spectroscopy (FTIR) monitoring to safely conduct the reaction is featured.