Journal
MOLECULES
Volume 14, Issue 5, Pages 1860-1868Publisher
MDPI
DOI: 10.3390/molecules14051860
Keywords
alkylation; quinazoline-2,4-dione; antihypertensive activity; microwaves
Funding
- Consejo Nacional de Ciencia y Tecnologia in Mexico (CONACYT) [SEP-2004-CO1-47835]
- Direccion General de Educacion Superior Tecnologica (DGEST)
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Alkylation is a very important chemical reaction which modifies the biological properties of drugs. Quinazolinedione derivatives are of considerable interest due to their wide array of pharmacological properties. We now report application of a practical alkylation procedure to several quinazolinediones, including pelanserine (5f), which shows antihypertensive properties, 1-methyl-3-(2'-phenylethyl)-1H,3H-quinazoline-2,4-dione (1ab) and 1-methyl-3-[2'-(4'-methoxyphenyl)ethyl]-1H,3H-quinazoline-2,4-dione (1ae), which had been isolated from natural sources. The alkylation was optimized using dimethyl and diethyl carbonates under microwave irradiations.
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