A Scalable Synthesis of (±)-2-Oxoclopidogrel

As a precondition for detailed pharmacological investigations, an effcient chemical method tor the conversion ot the antiplatelet drug clopidogrel into its first metabolite 2-oxoclopidogrel was developed. The one-pot procedure, which can easily be performed on a gram scale, exploits the selective borylation of a dianionic intermediate derived from clopidogrel with subsequent oxidative workup.