Methyl groups are widely found in small molecule drugs and play a crucial role. A large number of studies have shown that introducing methyl groups at specific sites of candidate drugs can improve the metabolic stability of the drug, shorten the half-life, and may also improve drug solubility, target selectivity, and even change the effect of the drug, such as turning an agonist into an antagonist. . When the hydrogen atom of the methyl group is replaced with a deuterium atom, it can not only be used to clarify the mechanism of drug action, slow down drug metabolism, and increase drug activity, but can also inhibit the configuration conversion of the drug, thereby improving the stability of its enantiomers and reducing the Drug toxicity.

Since traditional methylation strategies can only achieve a single methylation, and introducing deuterated methyl groups into molecules often requires the use of expensive deuterated methylation reagents, Professor Zhou Qianghui of Wuhan University developed a method based on the Catellani reaction. Modular dual-tasked C-H Methylation strategy (Dual-Tasked C-H Methylation) [1][1]

Zhou Qianghui, professor and doctoral supervisor, graduated from the School of Chemistry and Molecular Engineering of Peking University in 2005 with a bachelor's degree. His supervisors were Professor Wu Jinguang and Associate Professor Li Weihong. He graduated from the Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences in 2010 with a doctorate in science. His supervisor was Professor Ma Dawei; from 2011 to 2015, he engaged in postdoctoral research at Scripps Research Institute in the United States, and his co-supervisor was Professor Phil S. Baran. From 2015 to present, he serves as a professor at the School of Chemistry and Molecular Sciences of Wuhan University. Professor Zhou Qianghui has been committed to the efficient total synthesis of bioactive molecules, green drug process development, goal-oriented and structural diversity-oriented innovative synthesis methodology research, and related cross-research in chemical biology and medicinal chemistry. Professor Zhou Qianghui was funded by the National Natural Science Foundation of China's Outstanding Youth Science Fund Project, and has won the Outstanding Youth (Faculty) of Wuhan University (2023), the WuXi AppTec Life Chemistry Research Award (2022), and the Hubei Province Chemistry and Chemical Engineering Youth Innovation Award (2019) and Thieme Chemistry Journals Award (2017), and was selected into the National High-Level Talent Youth Project (2015). In terms of academic part-time work, he serves as the deputy secretary-general of the Process Chemistry Committee of the Chinese Chemical Society and a young editorial board member of Science of Synthesis, Green Synth. Catal. and "Organic Chemistry".

Bailingwei exclusively supplies a series of deuterated methylated aromatics developed by Professor Zhou Qianghui of Wuhan University, with high purity and diverse structures, which facilitates research in the field of medicinal chemistry!

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References

1. Gao Q, Shang Y, Song F, et al. Modular dual-tasked C–H methylation via the Catellani strategy[J]. Journal of the American Chemical Society, 2019, 141(40): 15986-15993.