Experimental chemical study demonstrates a scalable synthesis of the oxepanoproline fragment shared by novel antibiotics, highlighting streamlined production of clinical drug candidates.
A new, more scalable route for the synthesis of the common oxepanoproline southern fragment of the antibiotic candidates iboxamycin, cresomycin, and BT-33 is presented. A key transformation in the route is a diastereoselective TiCl 4 -mediated conjugate addition of an allylsilane to an Evans N -acryloyloxazolidinone, followed by syn -aldol addition of the resultant titanium enolate to ( R )-Garner’s aldehyde, which assembles all the stereocenters within the target molecule in a single operation.
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Wu et al. (2025) studied this question.
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