Pladienolide is a complex type I polyketide isolated from Streptomyces platensis that displays cytotoxic spliceosome modulating activity. Two of its analogues, E7107 and H3B-8800, have entered into clinical trials for the treatment of myeloid malignancies harboring splicing factor mutations. Herein, we report a 10-step total synthesis of pladienolide B, which bears 10 stereogenic centers, employing alcohol-mediated syn- and anti-diastereoselective carbonyl crotylations as key transformations.

10-Step total synthesis of spliceosome modulator pladienolide B

ACS Spring 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.