Synthesis of metabolically blocked paclitaxel analogues

  • Bioorg Med Chem Lett. 2001 Mar 26;11(6):809-10. doi: 10.1016/s0960-894x(01)00066-x.
M D Wittman  1 ,  T J Altstadt ,  C Fairchild ,  S Hansel ,  K Johnston ,  J F Kadow ,  B H Long ,  W C Rose ,  D M Vyas ,  M J Wu ,  M E Zoeckler
Affiliations
  • 1. Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492-7660, USA. [email protected]
Abstract

The stereospecific syntheses of the metabolically blocked 6-alpha-F, Cl, Br paclitaxel, and 6-alpha-F-10-acetyldocetaxel are described and in vitro and in vivo activity is presented.