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

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 prese...

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Bibliographic Details
Published in:Organic process research & development Vol. 13; no. 4; pp. 716 - 728
Main Authors: Pesti, Jaan, Chen, Chien-Kuang, Spangler, Lori, DelMonte, Albert J, Benoit, Serge, Berglund, Derek, Bien, Jeffrey, Brodfuehrer, Paul, Chan, Yeung, Corbett, Elisabeth, Costello, Carrie, DeMena, Paul, Discordia, Robert P, Doubleday, Wendel, Gao, Zhinong, Gingras, Stephane, Grosso, John, Haas, Oscar, Kacsur, David, Lai, Chiajen, Leung, Simon, Miller, Melanie, Muslehiddinoglu, Jale, Nguyen, Nina, Qiu, Jun, Olzog, Martina, Reiff, Emily, Thoraval, Dominique, Totleben, Michael, Vanyo, Dale, Vemishetti, Purushotham, Wasylak, John, Wei, Chenkou
Format: Journal Article
Language:English
Published: American Chemical Society 17-07-2009
Online Access:Get full text
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Summary: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.
ISSN:1083-6160
1520-586X
DOI:10.1021/op900065c