PARTIAL HYDROLYSIS PRODUCTS OF PCL5 & POCL3AS POSSIBLE PHOSPHORYLATING AGENTS

POCl 3是一种主要的商业磷酸化试剂， 合成包括生物制品在内的多种产品。 好久不见 认识到向POCl 3中加入水会显著改变 它的磷酸化性质，虽然活性的身份， 如此产生的试剂仍然不确定。 我们已经开发出一种新 研究PCl 5或POCl 3水解产物的方法 原位，使用在18-O水中的有限水解，然后完全水解， 在普通水中水解。 这些研究提供了信息， 原位水解过程的机理和动力学， 还发现存在磷氯酸，H2 PO 3CL， 迄今未检测到的水解中间体和可能的候选物， 部分水解混合物中的活性磷酸化试剂。

POCl3 is a major commercial phosphorylating agent used to synthesize numerous products including biologicals. It has been long recognized that the addition of water to POCl3 dramatically changes its phosphorylating properties although the identity of the active reagent so generated remains uncertain. We have developed a new method for studying the hydrolysis products of PCl5 or POCl3 generated in situ, using limited hydrolysis in 18-O water, followed by complete hydrolysis in normal water. These studies have provided information on the mechanism and kinetics of the in situ hydrolysis process and also revealed the presence of phosphorochloridic acid, H2PO3CL, a hitherto undetected hydrolytic intermediate and a likely candidate as the active phosphorylating reagent in partial hydrolysis mixtures.