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Vicinal difunctionalization of nitriles: modular construction of N-alkyl amidines and late-stage modification.
- Source :
- New Journal of Chemistry; 7/14/2024, Vol. 48 Issue 26, p11834-11843, 10p
- Publication Year :
- 2024
-
Abstract
- Through vicinal difunctionalization of nitriles, a successful, innovative strategy for the synthesis of N-alkyl amidines is developed. This methodology capitalizes on commercially available nitriles, alcohols, and sulfonamides. The activation of alcohols by trifluoromethanesulfonic anhydride (Tf<subscript>2</subscript>O) plays a pivotal role throughout the entire reaction process. In comparison to existing amidine synthesis methods, this strategy showcases notable advantages, including the avoidance of toxic and hazardous azides, the exclusion of transition metal catalysts, and the use of mild reaction conditions. Importantly, this methodology provides an effective approach for late-stage modification of complex molecules and drugs, holding promise for the construction of molecular libraries in drug discovery. [ABSTRACT FROM AUTHOR]
- Subjects :
- AMIDINES
MODULAR construction
TRANSITION metal catalysts
NITRILES
DRUG discovery
Subjects
Details
- Language :
- English
- ISSN :
- 11440546
- Volume :
- 48
- Issue :
- 26
- Database :
- Complementary Index
- Journal :
- New Journal of Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 178184299
- Full Text :
- https://doi.org/10.1039/d4nj02051k