One-pot microwave assisted preparation of pyrazoloquinazolinone libraries
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Updated: Aug 27, 2026

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Thomas E Vasquez1, Thomas Nixey, Balan Chenera
1Medicinal Chemistry Technologies, Chemistry Research and Development, AMGEN, One AMGEN Center Drive, Thousand Oaks, CA 91320, USA.
Abstract:
The novel solution-phase synthesis of an array of biologically relevant pyrazoloquinazolinones in a simple microwave driven one pot procedure is revelaed. Transformations are carried out in good to excellent yield by condensation of alpha-cyano-ketones and 2-hydrazino-benzoic acids. Subsequent microwave irradiation affords pyrazoloquinazolinones with six points of potential diversification. The protocol described represents a very attractive solution phase procedure for the rapid generation of arrays of such functionalized cores, further demonstrating the growing importance of economic and enabling complexity generating chemistries in the lead discovery arena.
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