Scaled-up synthesis of discodermolide
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SOME 60 G OF (+)-DISCODERmMOLIDE, a potent inhibitor of tumor cell growth, has been prepared in a 39-step synthesis by the Novartis Chemical & Analytical Development Group in Basel, Switzerland. The synthetic material is now undergoing Phase I clinical trials for pancreatic cancer at the Cancer Therapy & Research Center in San Antonio, Texas. "The large-scale total synthesis of such a complex natural product in such quantities was a first for Novartis and probably the entire pharmaceutical industry" says Novartis principal scientist Stuart J. Mickel, who played a significant part in the largescale synthesis effort. The synthesis is spectacular, according to Steven V. Ley, chemistry professor at the University of Cambridge, England. "It's probably the best piece of synthetic work to come out from an industrial company" he comments. "The ability to make something at this level of complexity as opposed to extracting it from natural product sources illustrates the power of modern synthetic ...