Alternative Synthesis and the Determination of Absolute Configuration of Docetaxel, an Anticancer Drug

Abstract

A simple, efficient, and alternative synthetic route for docetaxel with better control on the protection–deprotection sequence has been developed. The process is easily scalable and commercially viable, and critical impurities can be controlled efficiently. For the first time, absolute configuration of docetaxel was determined unambiguously by single-crystal x-ray diffraction.

GRAPHICAL ABSTRACT

Keywords:

• Absolute configuration
• anticancer
• 10-deacetyl baccatin III
• docetaxel and non-small cell lung cancer (NSCLC)

ACKNOWLEDGMENTS

The authors thank the management of Dr. Reddy's Laboratories Ltd. for supporting this work, and support from HPAI R&D and Discovery Research colleagues is highly appreciated.

Notes

^a ND, not detected.

DRL Communication No. IPDO IPM-0021.