cas 42465-69-0, 1-(2-Amino-3,4,5-trimethoxyphenyl)ethanone | Articles data ｜lookchem

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42465-69-0

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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.
Bandurco, Victor T.,Schwender, Charles F.,Bell, Stanley C.,Combs, Donald W.,Kanojia, Ramesh M.,et al.
p. 1421 - 1426
(2007/10/02)

Quino[1,2-c]quinazolines. I. Synthesis of quino[1,2-c]quinazolinium derivatives and the related indazolo[2,3-a]quinoline derivatives as analogs of the antitumor benzo[c]phenanthridine alkaloids
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Phillips,Castle
p. 1489 - 1495
(2007/10/02)

More Articles about upstream products of 42465-69-0

54173-39-6
2-nitro-3,4,5-trimethoxyacetophenone

More Articles about downstream products of 42465-69-0

76787-19-4
2-formamido-3,4,5-trimethoxyacetophenone

Chemical Properties

Boiling Point: 354°Cat760mmHg
Flash Point:162.3°C
Density: 1.153g/cm³
Storage Temp.:2-8°C(protect from light)
Vapor Pressure: 0mmHg at 25°C

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