Heterocycles
are the backbone of modern medical chemistry and drug
development. The derivatization of “an olefin” inside
aromatic rings represents an ideal approach to access functionalized
saturated heterocycles from abundant aromatic building blocks. Here,
we report an operationally simple, efficient, and practical method
to selectively access hydrosilylated and reduced N-heterocycles from
bicyclic aromatics via a key diradical intermediate. This approach
is expected to facilitate complex heterocycle functionalizations that
enable access to novel medicinally relevant scaffolds.
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