| 摘要 |
<p>Quinazolinone derivs with antiphlogistic properties.. G3A. are of formula (I): (where R = H, F, Cl, Br, alkyl with 1 to 5C, alkoxy or alkylthio with 1 to 4C, NO2, CN or CF3; n = 1 or 2, and in the latter case, the two R's may be same or different; R1 = alkyl with 1 to 5C, allyl or propargyl; and R2 = phenyl opt. substd. with one or two F, Cl, Br, alkyl, or alkoxy gps. or by one CF3 group) and are prepared (a) from appropriate aminobenzophenoneimines, (esp. 2-isopropyl-amino-4-methylbenzophenonimine, II), provided that R1 is not tert-alkyl, by cyclisation with methyl or pref. ethyl chlorocarbonate at 60-100 degrees C in the presence of an inert solvent and a base; or with lower alkyl carbamates, particularly excess urethane, and a Lewis acid at 160-80 degrees; or with 1,1'-carbonyldiimidazole in an inert solvent at 60-90 degrees; or with phosgene in the presence of a base and an inert solvent at 10-30 degrees; or (b) corresp. 3,4-dihydroquinazolinones are oxidised with MnO2 or MnO4 at 15-30 degrees, or the analogous thiones are hydrolysed with aqueous alkali at 80-120 degrees; or 3,4-dihydroquinazoline-2-thiones are treated with MnO4 at 0-60 degrees. The products (I) have valuable pharmacological properties, and can be used orally or parenterally in pharmaceutical preparations to reduce inflammation; cpds. such as (II) are also excellent analgetics.</p> |
