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Molecules 2009, 14(5), 1860-1868; doi:10.3390/molecules14051860

Alkylation of 2,4-(1H,3H)-Quinazolinediones with Dialkyl Carbonates Under Microwave Irradiations

1, 2,* , 1, 3, 1 and 3
1 Centro de Graduados e Investigación en Química, Instituto Tecnológico de Tijuana. C.P. 1166. Tijuana, B.C. 22000, Mexico 2 Instituto Nacional de Investigaciones Nucleares, Departamento de Química. Carretera México Toluca S/N, La Marquesa, Ocoyoacac, D.F. C.P. 52750, Mexico 3 Facultad de Química, Universidad Autónoma de Baja California, Calzada Tecnológico #14418, Mesa de Otay. Tijuana, B.C, C.P. 22390, Mexico
* Author to whom correspondence should be addressed.
Received: 16 March 2009 / Revised: 6 April 2009 / Accepted: 9 April 2009 / Published: 20 May 2009
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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]-lH,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.
Keywords: alkylation; quinazoline-2; 4-dione; antihypertensive activity; microwaves alkylation; quinazoline-2; 4-dione; antihypertensive activity; microwaves
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Rivero, I.A.; Guerrero, L.; Espinoza, K.A.; Meza, M.C.; Rodríguez, J.R. Alkylation of 2,4-(1H,3H)-Quinazolinediones with Dialkyl Carbonates Under Microwave Irradiations. Molecules 2009, 14, 1860-1868.

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