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assembly modification strategy. DMC was served not only as a
methylating reagent, but also as a base to promote the
transmetalation of boronic acids. Divergent functionalized
sulfones libraries were efficiently established through the
present
transformation.
Late-stage
modifications
of
pharmaceuticals were achieved efficiently via this protocol.
Further explorations of sulfone-containing molecules employing
the multicomponent cross-coupling strategy for drug discovery
are in progress in our laboratory.
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Acknowledgements
We acknowledge financial support from the National Key
Research
and
Development
Program
of
China
(2017YFD0200500), NSFC (21722202, 21672069, 21871089 for
M.W.), S&TCSM of Shanghai (Grant 18JC1415600), Professor
of Special Appointment (Eastern Scholar) at Shanghai
Institutions of Higher Learning, and National Program for
Support of Top-notch Young Professionals.
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Keywords: Sulfonemethylation • dimethyl carbonate • sodium
metabisulfite • pharmaceutical • late-stage modification
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