One-Pot Synthesis of β‑Hydroxysulfones and Its Application in the Preparation of Anticancer Drug Bicalutamide

An
efficient one-pot multistep strategy has been developed, comprising
auto-oxidative difunctionalization of alkenes, oxidation of sulfides,
and a further reduction of peroxides for the synthesis of complex
β-hydroxysulfone derivatives from phenthiols and alkenes. This
method has several advantageous characteristics, including readily
available substrates, low-cost and environmental benign reagents,
nontoxic and renewable solvents, and mild reaction conditions. The
application of this transformation to the multigram-scale preparation
of the anticancer drug bicalutamide is accomplished.