Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
本文公开了一种通过在无
水反应条件下氧化药物的1-酰基-烷基衍
生物来合成药物的1-(酰氧基)-烷基前药衍
生物的方法。该方法通常具有立体选择性,产率高,不需要使用活性中间体和/或有毒化合物,并且容易扩大规模。