Genentech's THIOMAB Antibiotic Conjugate (TAC) is the combination of a targeted large molecule biologic with a potent anti-infective payload connected via a linker. A <i>Staphylococcus aureus</i>-targeting TAC candidate has been advanced into the clinic with the small molecule linker-antibiotic resulting from a novel process chemistry approach.  The small molecule is a highly complex, semi-synthetic quaternary salt construct with stability and solubility challenges. An efficient and robust chemical process, including a key transformation in continuous flow, has been developed for this unusual small molecule to deliver the linker-drug in good yield and high purity. The innovative continuous oxidation process with an elaborate natural product component yields the key intermediate to enable further construction by successive displacement reactions, all without protecting groups.

Arming an anti-<i>Staph. aureus</i> THIOMAB antibiotic conjugate (TAC) with process chemistry

256th National Meeting (2018)

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Arming an anti-Staph. aureus THIOMAB antibiotic conjugate (TAC) with process chemistry