Nielsen K K, Senning A
Department of Organic Chemistry, University of Aarhus, Denmark.
Acta Chem Scand (Cph). 1990 Oct;44(9):952-6. doi: 10.3891/acta.chem.scand.44-0952.
A series of new 2-substituted 2-methyl-4H-1,3-benzodioxin-4-ones 1 have been synthesized and fully characterized. This study involves fifteen compounds of which fourteen are orthoesters, containing tertiary aliphatic alkoxy groups. One compound contains a tert-butylperoxy group and one a 3 beta-cholesteryloxy group in the 2-position. The hydrolysis of these compounds 1 was followed in enzymatic and non-enzymatic media to clarify whether they are true prodrugs of aspirin. Two compounds 1 were additionally tested in vivo as potential topical keratolytics.
一系列新的2-取代-2-甲基-4H-1,3-苯并二恶英-4-酮1已被合成并进行了全面表征。本研究涉及十五种化合物，其中十四种是原酸酯，含有叔脂肪族烷氧基。一种化合物在2-位含有叔丁基过氧基，一种含有3β-胆甾醇氧基。在酶促和非酶促介质中跟踪这些化合物1的水解，以阐明它们是否是阿司匹林的真正前药。另外对两种化合物1进行了体内潜在局部角质层分离剂的测试。
