Experimental study demonstrates efficient synthesis of deuterated amino acids in diverse molecular scaffolds, highlighting broad utility in medicinal chemistry.
-Hantzsch ester as the deuterium source, this reaction attains remarkable deuteration efficiency (> 99% deuteration). It enables the synthesis of N-α-deuterated amino acid motifs with a wide range of functionality, as evidenced by over 130 examples. The method exhibits compatibility with diverse substrates, such as amino acids, peptides, drug molecules, and natural products bearing different substituents. Moreover, the application of this strategy in the synthesis of DNA-tagged N-α-deuterated amino acids/peptides has been demonstrated. This work offers an efficient and innovative solution for deuterated amino acid chemistry and holds substantial application potential in organic synthesis, medicinal chemistry, and chemical biology.
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Li et al. (2025) studied this question.
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