The increasing demand for deuterium‐labeled amino acids and derivatives has heightened interest in direct hydrogen/deuterium exchange reactions of free amino acids. Existing methods, including biocatalysis and metal catalysis, typically require expensive deuterium sources or excessive use of deuterium reagents and often struggle with site selectivity. In contrast, our pioneering binary catalysis system, employing benzaldehyde and Cs2CO3 in the presence of inexpensive D2O with minimal stoichiometric quantities, facilitates efficient hydrogen/deuterium exchange at the α‐position of amino acids without the need for protecting groups in the polar aprotic solvent DMSO. The process is highly compatible with most natural and non‐natural α‐amino acids and derivatives, even those with potentially reactive functionalities. This advancement not only addresses the cost and efficiency concerns of existing methods but also significantly broadens the applicability and precision of deuterium labeling in biochemical research.

中文翻译：

---

游离 α-氨基酸及其衍生物的二元催化氢/氘交换


对氘标记氨基酸及其衍生物的需求不断增加，引起了人们对游离氨基酸直接氢/氘交换反应的兴趣。现有的方法，包括生物催化和金属催化，通常需要昂贵的氘源或过量使用氘试剂，并且常常难以实现位点选择性。相比之下，我们开创性的二元催化系统，在廉价的 D2O 存在下以最小的化学计量使用苯甲醛和 Cs2CO3，促进氨基酸 α 位的有效氢/氘交换，而不需要极性非质子溶剂 DMSO 中的保护基团。该过程与大多数天然和非天然 α-氨基酸及衍生物高度兼容，甚至是那些具有潜在反应性功能的氨基酸和衍生物。这一进步不仅解决了现有方法的成本和效率问题，而且显着拓宽了氘标记在生化研究中的适用性和精度。