A metabolic inhibitor blocks cellular fucosylation and enables production of afucosylated antibodies.

The fucosylation of glycoproteins regulates diverse physiological processes. Inhibitors that can control cellular levels of protein fucosylation have consequently emerged as being of high interest. One area where inhibitors of fucosylation have gained significant attention is in the production of afucosylated antibodies, which exhibit superior antibody-dependent cell cytotoxicity as compared to their fucosylated counterparts.

Palladium-Catalyzed Allylation/Benzylation of H-Phosphinate Esters with Alcohols.

The Pd-catalyzed direct alkylation of -phosphinic acids and hypophosphorous acid with allylic/benzylic alcohols has been described previously. Here, the extension of this methodology to -phosphinate esters is presented. The new reaction appears general, although its scope is narrower than with the acids, and its mechanism is likely different.