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

Autor: Derek Berglund, Jeffrey T. Bien, John Wasylak, Purushotham Vemishetti, David J. Kacsur, Jun Qiu, Oscar W. Haas, Chien-Kuang Chen, Yeung Y. Chan, Carrie A. Costello, Lori Spangler, Emily A. Reiff, Jale Muslehiddinoglu, Dale Vanyo, Stephane Gingras, Jaan A. Pesti, Nina Nguyen, Albert J. DelMonte, John A. Grosso, Chiajen Lai, Simon Leung, Wendel W. Doubleday, Michael J. Totleben, Paul Demena, Elisabeth Corbett, Martina Olzog, Dominique Thoraval, Serge Benoit, Melanie Miller, Robert P. Discordia, Zhinong Gao, Paul R. Brodfuehrer, Chenkou Wei
Rok vydání: 2009
Předmět:
Zdroj: Organic Process Research & Development. 13:716-728
ISSN: 1520-586X
1083-6160
DOI: 10.1021/op900065c
Popis: 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.
Databáze: OpenAIRE