AI Article Synopsis
- The text discusses an efficient method for synthesizing a variety of difluoromethylphosphonates, including aryl and heteroaryl types, using TMSCF2PO(OEt)2 and copper salts.
- The method is notable for its tolerance to various functional groups and operates under mild conditions, yielding good to excellent results.
- This represents the first general synthetic approach to this significant class of fluorinated compounds, which are important due to their stability as phosphate substitutes in biological applications.
Article Abstract
A general and efficient access to aryl, heteroaryl, vinyl and alkynyl difluoromethylphosphonates is described. The developed methodology using TMSCF2PO(OEt)2, iodonium salts and a copper salt provided a straightforward manifold to reach these highly relevant products. The reaction proved to be highly functional group tolerant and proceeded under mild conditions, giving the corresponding products in good to excellent yields. This method represents the first general synthetic route to this important class of fluorinated scaffolds, which are well-recognized as in vivo stable phosphate surrogates.
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| http://dx.doi.org/10.1002/anie.201507130 | DOI Listing |
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