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Whipping Phosphorus into Chiral Shape

有机合成与工艺文献分享 2025-08-04 07:05
文章摘要
本文介绍了Merck研究团队在有机合成领域的一项突破性工作，他们开发了一种高效的不对称催化合成方法，用于制备手性磷酸盐和磷酰胺。研究背景是传统的手性磷化合物合成方法效率低下且步骤繁琐。研究目的是通过改进催化剂设计，实现更高的立体选择性和产率。团队基于上海交通大学张万斌课题组先前开发的双氢吡咯并咪唑骨架催化剂，通过计算建模、信息学和动力学分析优化催化剂性能，最终设计出能高效形成磷手性中心的催化剂。研究结论表明，改进后的催化剂在制备前核苷酸药物候选物时表现出优异的性能，磷中心的立体选择性达到99:1，产率达92%，完全满足MK-3682药物的生产要求。
Whipping Phosphorus into Chiral Shape
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