Syntheses of Cyclopropyl Analogues of Disorazoles A and B and Their Thiazole Counterparts.

08:00 EDT 2nd October 2018 | BioPortfolio

Summary of "Syntheses of Cyclopropyl Analogues of Disorazoles A and B and Their Thiazole Counterparts."

Modular syntheses of disorazoles A and B analogues in which the epoxide moieties of the natural products were replaced with cyclopropyl units have been achieved. Targeted as part of a structure-activity relationships study, these syntheses were successfully extended to the thiazole counterparts of these analogues. The retrosynthetically defined fragments were assembled through Yamaguchi esterification, Cu/Pd-catalyzed cross-coupling, Yamaguchi macrolactonization, and Cu-catalyzed cross-coupling as the key reactions. Further synthetic and biological investigations of such analogues are expected to lead to the discovery and development of potential payloads for antibody-drug conjugates as targeted cancer therapies.


Journal Details

This article was published in the following journal.

Name: The Journal of organic chemistry
ISSN: 1520-6904


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