Abstract：
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.
摘要：
对氘标记的氨基酸和衍生物的不断增长的需求增加了对游离氨基酸的直接氢/氘交换反应的兴趣。现有方法,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，并且经常需要位点选择性。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量使用苯甲醛和Cs2CO3，在不需要极性非质子溶剂DMSO中的保护基团的情况下,促进在氨基酸的α-位处的有效氢/氘交换。该方法与大多数天然和非天然α-氨基酸及其衍生物高度兼容，甚至那些具有潜在反应性官能团的。这种进步不仅解决了现有方法的成本和效率问题，而且显着扩大了氘标记在生化研究中的适用性和准确性。
