Professor Jing Li from School of Chemistry, and Xi'an Key Laboratory of Sustainable Energy Materials Chemistry, Xi'an Jiaotong University (XJTU) has developed a novel synthesis method: by activating nitroalkanes using elemental sulfur to generate thioacylation reagents in situ. Through the interaction of these agents with amines, they have achieved the efficient synthesis of thioamides. This method can also be extended to the enantioselective synthesis of thiopeptides (Figure 1).

Furthermore, this strategy has been applied to functionalize various drug molecules and biologically active compounds with thioamide moieties. The total synthesis of the natural antibiotic closthioamide, which contains multiple thioamide motifs, has also been accomplished using this approach.

Figure 1.

This innovative approach can convert inexpensive, non-toxic, and odorless sulfur into sulfur-containing functional molecules. It not only offers an effective solution to the utilization of sulfur, but also opens up new avenues for the development of sulfur-containing functional molecules.

The research findings were recently published in Nature Communications, with the lead author of the study as Dr. Wang Xiaonan. The collaborators include Professor Xu Silong from XJTU, Professor Martin Lear from the University of Lincoln in the United Kingdom, and researcher He Wangxiao from the First Affiliated Hospital of XJTU.

The research was supported by grants from the National Natural Science Foundation of China, the Shaanxi Province Youth Talent Program, and the Analytical Testing Center of XJTU.