Development of on-DNA Formation of Benzofuran for DNA-Encoded Library Synthesis
Ayun Luo,
Hongxia Zhou,
Xiuming Wang
et al.
Abstract:Using
a novel homologation–heterocyclization cascade, the
on-DNA synthesis of benzofurans from aldehydes has been developed.
The methodology, based on an innovative use of the Seyferth–Gilbert
homologation, followed by a high yielding Sonogashira coupling in
situ intramolecular cyclization one-pot, two-step reaction, provides
a powerful and unique pathway for DNA-encoded library (DEL) synthesis
of a wide array of pharmaceutically relevant benzofuran-based scaffolds.
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