Bodor N, Sloan K B, Kuo Y N, Higuchi T
J Pharm Sci. 1978 Aug;67(8):1045-50. doi: 10.1002/jps.2600670806.
7-Acyl- and 7,7'-acylditheophylline derivatives were prepared from the reaction of theophylline with acid chlorides. In addition, a novel synthesis of these compounds was developed, which proceeds through an acylonium ion generated under mild conditions. The physical properties and stability of the derivative of choice, 7,7'-succinylditheophylline, depend on the synthetic procedure employed. This compound is a useful controlled-release prodrug of theophylline.
7-酰基和7,7'-酰基二茶碱衍生物是由茶碱与酰氯反应制备而成。此外,还开发了一种新型的这些化合物的合成方法,该方法通过在温和条件下生成的酰鎓离子进行。所选衍生物7,7'-琥珀酰二茶碱的物理性质和稳定性取决于所采用的合成方法。该化合物是一种有用的茶碱控释前药。