Synthesis and Antitumor Activity of Novel 2-(Thymin-1′-ylmethoxy)ethyl Alkyl Sulfides and Their Oxidation Products

A series of novel 2-(thymin-1′-ylmethoxy)ethyl alkyl sulfides have been synthesized in three steps from thymine. They have been oxidized into sulfoxide and sulfone derivatives by means of NaIO ₄ and H ₂ O ₂ 30%/diethyl azodicarboxylate (DEAD), respectively, in high yields. All products were characterized by ¹ H NMR and IR spectra and elemental analyses. The preliminary bioassay indicates that the compound 6g exhibited potential antitumor activity.

Keywords:

• Diethyl azodicarboxylate
• sulfides
• sulfones
• sulfoxides
• thymine

Acknowledgments

This project was supported by National Natural Science Foundation of China (No. 20172027).