Journal
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
Volume 12, Issue -, Pages 702-715Publisher
BEILSTEIN-INSTITUT
DOI: 10.3762/bjoc.12.70
Keywords
alpha-lithiation; C-H functionalization; heterocycle; photoredox catalysis; piperazine
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Funding
- Purdue University
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Piperazine ranks within the top three most utilized N-heterocyclic moieties in FDA-approved small-molecule pharmaceuticals. Herein we summarize the current synthetic methods available to perform C-H functionalization on piperazines in order to lend structural diversity to this privileged drug scaffold. Multiple approaches such as those involving alpha-lithiation trapping, transitionmetal-catalyzed alpha-C-H functionalizations, and photoredox catalysis are discussed. We also highlight the difficulties experienced when successful methods for alpha-C-H functionalization of acyclic amines and saturated mono-nitrogen heterocyclic compounds (such as piperidines and pyrrolidines) were applied to piperazine substrates.
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