Abstract
An optimised synthesis of a hypoxia-activated anticancer prodrug related to the duocarmycin family of natural products is described. The improved 10-step synthesis increases the overall yield from 4.4% to over 40% while requiring just 2 chromatography-based purifications. The most significant improvements optimise the isomer distribution in a key chlorosulfonylation reaction, and facilitate the removal of tin residues from a tributyltin hydride-mediated radical reaction. Improved preparations of two side chains are also reported. The new method provides practical access to sufficient material to support advanced efficacy and toxicology assessments.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
