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

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journal contribution
posted on 17.07.2009 by Jaan Pesti, Chien-Kuang Chen, Lori Spangler, Albert J. DelMonte, Serge Benoit, Derek Berglund, Jeffrey Bien, Paul Brodfuehrer, Yeung Chan, Elisabeth Corbett, Carrie Costello, Paul DeMena, Robert P. Discordia, Wendel Doubleday, Zhinong Gao, Stephane Gingras, John Grosso, Oscar Haas, David Kacsur, Chiajen Lai, Simon Leung, Melanie Miller, Jale Muslehiddinoglu, Nina Nguyen, Jun Qiu, Martina Olzog, Emily Reiff, Dominique Thoraval, Michael Totleben, Dale Vanyo, Purushotham Vemishetti, John Wasylak, Chenkou Wei
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.