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The extreme structural diversity found in many natural products poses an extraordinary challenge to chemists trying to synthesize these molecules (1). Many natural products are available only in trace quantities from natural sources, making total or partial synthesis a necessity. For example, the drug Taxol, an anticancer natural product, is present only in minute quantities in the bark of Taxus brevifolia. A closely related compound, 10-deacetylbaccatin III, can be extracted from leaf clippings from Taxus baccata with no harm to the tree (2). During studies of the transformation of 10-deacetylbaccatin into Taxol, a compound was synthesized that turned out to be more soluble and twice as active as Taxol itself (3). This compound was developed into the drug Taxotere. Total and partial syntheses of bioactive natural products and derivatives also provide the driving force for the invention of new reactions with ever-increasing levels of efficiency and selectivity.
Peter E. Kündig (Thu,) studied this question.