Partial synthesis of major human metabolites of docetaxel

Article abstract of DOI:10.1016/S0040-4020(01)81761-0

The structures and synthesis of the four major human metabolites of docetaxel are reported. These metabolites, i.e. compounds 3, 4a,b and 5, are side-chain oxidation derivatives. They were prepared by partial synthesis from the previously described amino-taxoid 8 using mixed-carbonates as acylation reagents. In vitro biological activities are detailed.