Abstract
A versatile and practical “on-water” protocol was newly developed to synthesize quinazolinones using o-bromobenzonitrile as a novel starting material. Studies have found that air as well as water plays an important role in synthesis of quinazolinones. Further investigation indicated that dihydroquinazolinones can be prepared with this protocol under the protection of N2. The protocol can be extended to other substrates and various quinazolinones and dihydroquinazolinones were obtained. o-Bromobenzamide, o-aminobenzonitrile, and o-aminobenzamide were also evaluated as starting materials, and the results further proved the versatility of this protocol, especially towards dihydroquinazolinones.
Highlights
Quinazolinones and dihydroquinazolinons are important classes of nitrogen-containingQuinazolinones and dihydroquinazolinons are important classes of nitrogen-containing heterocycles with an array of biological activities such a antitumor [1,2], anti-inflammatory [3], heterocycles with an array of biological activities such an antitumor [1,2], anti-inflammatory [3], antibacterial [4,5], anticonvulsant [6], etc
“on-water” protocol protocol towards towards compounds containing a quinazolinone core, and o-bromobenzonitrile was explored as an alternative compounds containing a quinazolinone core, and o-bromobenzonitrile was explored as an alternative
We have newly developed a versatile and practical “on-water” protocol towards compounds containing a quinazolinone core, and o-bromobenzonitrile was explored as an alternative starting material
Summary
Quinazolinones and dihydroquinazolinons are important classes of nitrogen-containing heterocycles with an array of biological activities such a antitumor [1,2], anti-inflammatory [3], heterocycles with an array of biological activities such an antitumor [1,2], anti-inflammatory [3], antibacterial [4,5], anticonvulsant [6], etc. RVX-208 and balaglitazone, structurally structurally based on quinazolin-4(3H)-one (Figure 1), are under phase III clinical trials. The compound of compound of RVX-208 is developed for the treatment of cardiovascular diseases and lipid. RVX-208 is developed for the treatment of cardiovascular diseases and lipid metabolism disorders [7], metabolism disorders [7], while balaglitazone is developed for the treatment of type 2 diabetes [8].
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