George Pettit - Paradise Valley AZ, US Brian Orr - Del Mar CA, US Sylvie Ducki - Salford, GB
International Classification:
A61K031/665
US Classification:
514/099000
Abstract:
A new and efficient synthesis of the (+)-pancratistatin phosphate prodrug has been accomplished. Selective protection (tetraacetate ) of (+)-pancratistatin () was followed by phosphorylation (to ) with dibenzyl chlorophosphite (prepared in situ from dibenzyl phosphite). Cleavage of the acetate (with sodium methoxide) and benzyl (by hydrogenolysis) protecting groups followed by concomitant reaction with two equivalents of sodium methoxide afforded good yield of disodium (+)-pancratistatin phosphate (). Further increases in yields of the prodrug () were realized by avoiding heat in the final purification steps. Fourteen (-) additional metal and ammonium derived phosphate prodrugs were also synthesized.
Those playing the disciples in the event included Brian Orr as Nathaniel, Doug Winter as James the Less, Andy Acord as Andrew, Lanny Stocke as Peter, Scott Riley as Judas, Daniel Drury as John, Brady Wooten as James, Doug Hays as Thomas, Grant Gee as Philip, Tom Sutton as Matthew, Henry Bob Haley as