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The metal-free cascade transformation of geldanamycin benzoquinone core is proposed at relatively mild conditions. This approach yields new benzoxazole ansamycin antibiotics and enables their functionalization in an atom-economic manner, irrespective of the type of amine used. The analysis of the heterocyclization course reveals the dependence of its rate on the nature of the -substituent within the benzylamine moiety (EDG/EWG) and the strength of the base. The reduction of the ansamycin core enables an increase in anticancer potency and selectivity.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10337034 | PMC |
| http://dx.doi.org/10.1021/acs.joc.3c00493 | DOI Listing |
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