Alkylation of 24-(1H3H)-Quinazolinediones with Dialkyl Carbonates Under Microwave Irradiations

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.