Development of Synthetic Methodology Suitable for the Radiosynthesis of Combretastatin A-1 (CA1) and Its Corresponding Prodrug CA1P†

…, JJ Hall, BL Nguyen, R Guddneppanavar…

Index: Shirali, Anupama; Sriram, Madhavi; Hall, John J.; Nguyen, Benson L.; Guddneppanavar, Rajsekhar; Hadimani, Mallinath B.; Ackley, J. Freeland; Siles, Rogelio; Jelinek, Christopher J.; Arthasery, Phyllis; Brown, Rodney C.; Murrell, Victor Leon; McMordie, Austin; Sharma, Suman; Chaplin, David J.; Pinney, Kevin G. Journal of Natural Products, 2009 , vol. 72, # 3 p. 414 - 421

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Citation Number: 23

Abstract

Synthetic methodology has been established suitable for the preparation of combretastatin A- 1 (CA1) and its corresponding phosphate prodrug salt (CA1P) in high specific activity radiolabeled form. Judicious selection of appropriate phenolic protecting groups to distinguish positions on the A-ring from the B-ring of the stilbenoid was paramount for the success of this project. Methylation of the C-4′ phenolic moiety by removal of the tert- ...