Journal
ACS COMBINATORIAL SCIENCE
Volume 20, Issue 5, Pages 256-260Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acscombsci.8b00032
Keywords
ynoates; parallel synthesis; 7-arylpyrazolo[1,5-a]pyrimidin-5(4H)-ones; regioselective; orthoester; Sonogashira
Funding
- Pfizer Inc.
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A modular, two-pot assembly of 7-arylpyrazolo[1,5-a]pyrimidones from aryl/heteroaryl halides and aminopyrazoles in library format was developed. Sonogashira coupling of aryl bromides with triethyl orthopropiolate, followed by in situ orthoester hydrolysis, provides access to beta-aryl ynoates, which undergo regioselective cyclocondensation with aminopyrazoles. The ability to vary the C7 vector of 7-arylpyrazolo[1,5-cdpyrimidones in two steps using readily available (hetero)aryl halides significantly enhances synthetic access to this challenging vector.
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