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

Molecules

Ignacio Alfredo Rivero¹  Leticia Guerrero¹  Karla Alejandra Espinoza¹  Martha Cecilia Meza¹ 

[1] ¹Centro de Graduados e Investigación en Química, Instituto Tecnológico de Tijuana. C.P. 1166. Tijuana, B.C. 22000, Mexico

关键词: alkylation;    quinazoline-2;    4-dione;    antihypertensive activity;    microwaves;   

DOI  :  10.3390/molecules14051860

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
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.