A Parallel Approach to 7‑(Hetero)arylpyrazolo[1,5‑a]pyrimidin-5-ones
datasetposted on 04.04.2018 by Daniel C. Schmitt, Nootaree Niljianskul, Neal W. Sach, John I. Trujillo
Datasets usually provide raw data for analysis. This raw data often comes in spreadsheet form, but can be any collection of data, on which analysis can be performed.
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 β-aryl ynoates, which undergo regioselective cyclocondensation with aminopyrazoles. The ability to vary the C7 vector of 7-arylpyrazolo[1,5-a]pyrimidones in two steps using readily available (hetero)aryl halides significantly enhances synthetic access to this challenging vector.