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Maxime Bergeron Thomas Johnson Jean‐Franois Paquin 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2011,123(47):11308-11312
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《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2017,129(2):634-638
Terminal monofluoroalkenes are important structural motifs in the design of bioactive compounds, such as homeostasis regulators and mechanism‐based enzyme inhibitors. However, it is difficult to control the stereoselectivity of known carbonyl olefination reactions, and olefin metathesis is limited to disubstituted terminal monofluoroalkenes. Although sulfoximines have been used extensively in organic synthesis, reports on their use in carbonyl olefination reactions have not appeared to date. Herein, we report highly stereoselective carbonyl monofluoroolefination with a fluorosulfoximine reagent. The potential of this method is demonstrated by the synthesis of MDL 72161 and by the late‐stage monofluoromethylenation of complex molecules, such as haloperidol and steroid derivatives. 相似文献
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