Journal
ACS COMBINATORIAL SCIENCE
Volume 19, Issue 5, Pages 343-350Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acscombsci.7b00033
Keywords
tetrazolopiperidinone; isocyanide; multicomponent reaction; Ugi reaction; ammonia Ugi reaction; European Lead Factory
Funding
- NIH [2R01GM097082-05]
- Innovative Medicines Initiative [115489]
- European Union's Horizon Research and Innovation Programme under MSC ITN Accelerated Early Stage Drug Discovery (AEGIS) [675555]
- European Regional Development Fund of the Polish Innovation Economy Operational Program [POIG.02.01.00-12-023/08]
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Ammonia in the tetrazole Ugi variation together with alpha-amino acid methyl ester-derived isocyanides provides tetrazolopiperidinones in good to high yields in one pot. The scope and limitations of this reaction were investigated by performing >70 reactions. The scaffold is useful to fill high-throughput screening decks and in structure based drug design.
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