Journal
SCIENCE
Volume 367, Issue 6475, Pages 281-+Publisher
AMER ASSOC ADVANCEMENT SCIENCE
DOI: 10.1126/science.aay9501
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Funding
- NSFC [21632001, 21772002, 81821004]
- National Basic Research Program of China(973 Program) [2015CB856600]
- Drug Innovation Major Project [2018ZX09711-001]
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The Schmidt reaction has been an efficient and widely used synthetic approach to amides and nitriles since its discovery in 1923. However, its application often entails the use of volatile, potentially explosive, and highly toxic azide reagents. Here, we report a sequence whereby triflic anhydride and formic and acetic acids activate the bulk chemical nitromethane to serve as a nitrogen donor in place of azides in Schmidt like reactions. This protocol further expands the substrate scope to alkynes and simple alkyl benzenes for the preparation of amides and nitriles.
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