P-Heterocyclic building blocks: Utility in natural product synthesis

ORGN 22

Alan Whitehead and Paul R. Hanson. Department of Chemistry, University of Kansas, 1251 Wescoe Hall Dr, Lawrence, KS 66045
The synthetic utility of nonracemic phosphorus heterocycles (P-heterocycles) produced via ring-closing olefin metathesis (RCM) will be presented. We have demonstrated that phosphorus can be utilized for the rapid functionalization of RCM-generated cyclic allyl phostone motifs en route to P-chiral phosphonosugars. We now report a terminus differentiation strategy utilizing RCM for the desymmetrization of 1,3-anti-diols employing a phosphorus tether. The resulting bicyclic phosphorus framework contains a number of salient features, including endo- and exocyclic olefins for further synthetic manipulation and a temporary phosphorus tether (P-tether). The primary goal of this project is to evaluate the efficacy of these P-heterocyclic building blocks in application towards the development of 1,3-diol-containing synthons for target-directed synthesis. Initial efforts in our group are aimed at the heptalactone feigrisolide B. Feigrisolide B has been found to demonstrate high levels of antibacterial activity as well as moderate cytotoxic and antiviral properties.
 

New Reactions and Methodology
8:00 AM-12:00 PM, Sunday, March 28, 2004 Anaheim Convention Center -- 303A, Oral

Division of Organic Chemistry

The 227th ACS National Meeting, Anaheim, CA, March 28-April 1, 2004