Journal
ORGANIC CHEMISTRY FRONTIERS
Volume 8, Issue 11, Pages 2799-2819Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d1qo00032b
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Funding
- National Natural Science Foundation of China [81872723, 82073679]
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This review summarizes routine asymmetric synthetic methods for the effective and selective introduction of difluoromethyl groups into desired compounds, which is valuable for the synthesis of fluorine-containing compounds and for modulating the properties of organic compounds in drug design.
Difluoromethyl groups possess specific steric and electronic properties due to their slightly acidic C-H bonds and the natural characteristics of fluorine atoms, which allow them to act as chemically inert hydrogen-bond donors and then as surrogates in a wide assortment of important molecular recognition processes. As a result, the construction of chiral carbon centres bearing difluoromethyl groups is not only valuable for the synthesis of various fluorine-containing compounds, but also useful for the modulation of the properties of organic compounds in drug design. The scope of this review is to summarize routine asymmetric synthetic methods which enable the effective and selective introduction of difluoromethyl groups into the desired compounds.
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