92210-40-7

Upstream product

• 92210-39-4 6-(N-Carboethoxyamino)-2,3-dimethoxybenzaldehyde ethylene acetal 
• 2531-63-7 5,6-dimethoxy-2-nitrobenzaldehyde 
• 111042-36-5 2-Hydroxy-3-methoxy-6-nitrobenzaldehyde, sodium salt 
• 92210-38-3 6-Amino-2,3-dimethoxybenzaldehyde ethylene acetal 
• 92210-37-2 2,3-Dimethoxy-6-nitrobenzaldehyde ethylene acetal 
• 148-53-8 3-methoxy-2-hydroxybenzaldehyde 
• 2426-60-0 2-Hydroxy-3-methoxy-6-nitrobenzaldehyde benzenesulfonate 

Downstream Products

• 92210-41-8 5,6-dimethoxy-2(1H)-quinazolinone 
• 92210-43-0 5,6-dimethoxy-4-methyl-2(1H)-quinazolinone 

Relevant academic research and scientific papers

Synthesis and Cardiotonic Activity of a Series of Substituted 4-Alkyl-2(1H)-quinazolinones

The synthesis, cardiac fraction III cyclic nucleotide phosphodiesterase (PDE-III) inhibition, and positive inotropic activity of a series of 2(1H)-quinazolinones are reported.A general synthesis of the series involved the cyclization of 2-aminoacetophenones with potassium cyanate in acetic acid.Modifications at the 4-position of the quinazoline nucleus were best achieved by formation of the intermediate N1-acyl-N3-phenylurea from the substituted phenyl isocyanate and appropriate carboxamide.PPA was used to ring close to the quinazoline product.Generally the SAR for the series paralleled the five-point model previously published for PDE-III inhibition.The most active analogue of the series was 5,6-dimethoxy-4-methyl-2(1H)-quinazolinone (1) (ORF 16600), which had about twice the intravenous potency of amrinone.Compound 1 is currently under development as an orally active cardiotonic.

5,6-Dialkoxy-3,4-optionally substituted-2(1H)quinazolinones, composition and method of use

The synthesis of substituted quinazolinones is described. The novel quinazolinones are renal vasodilators and thereby increase renal blood flow, and are useful as cardiovascular agents.