梭曼抗体酶研究: Ⅰ.五配位氧膦烷半抗原的设计与合成及其水解稳定性研究

Studies on the catalytic antibodies against soman.Ⅰ. Design and synthesis of pentacoordinated phosphorus mimicking the transition state of soman hydrolysis as haptens. Hydrolysis of unsymmetrically substituted monocyclic oxyphosphoranes

目的：探索用化学免疫方法防治梭曼中毒。方法：对梭曼水解过渡态进行了模拟设计与合成，并对其水解过渡态作了有益的探讨。结果与讨论：我们发现，频哪基直接引入后，五配位氧膦烷Ⅱ的水解稳定性较差；并分离了两个水解产物：甲基膦酸的双酯和单酯。

Objective: To explore novel strategy for soman antidote by chemical immunization. Methods: Designing and synthesizing a series of unsymmetrically substituted monocyclic oxyphosphoranes to mimic the transition state of soman hydrolysis, studying the hydrolysis stability of the oxyphosphoranes by 31P NMR. Results: A series of monocyclic oxyphosphoranes were synthesized and two products of their hydrolysis, diester and monoester of methylphosphonic acid, were separated. Conclusion: The oxyphosphoranes with pinacolyl are liable to be hydrolyzed, and their reactive sites are the two less bulky ligands occupying the two perpendicular abonds.