ChemInform Abstract: Conformationally Restricted Paclitaxel Analogues: Macrocyclic Mimics of the “Hydrophobic Collapse” Conformation.
Abstract
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ChemInform Abstract
The synthesis of conformationally restricted macrocyclic taxol analogues designed to mimic the hydrophobically collapsed conformation is described. Key steps of the syntheses are an intramolecular Heck reaction and a macrolactonization under high dilution conditions, respectively. NMR analysis shows that compound (V) is a mixture of two atropisomers. The analogues do not show activity in a tubulin assembly assay.
