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

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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Veröffentlicht in:Organic process research & development 2009-07, Vol.13 (4), p.716-728
Hauptverfasser: 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: Artikel
Sprache:eng
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Zusammenfassung: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