The introduction of methyl groups into drug molecules can change their pharmacokinetic and pharmacological properties.This "magical methyl effectˮ makes methylation a very important reaction in the field of organic synthesis and pharmaceutical chemistry.In recent years, the transition metal-catalyzed coupling reaction and the organic reaction promoted by light or electricity have become the new strategies for methylation reaction.A series of cheap, low toxicity, high efficiency and wide applicability of methylating reagents have been developed.Among them, dimethyl sulfoxide (DMSO), as a kind of solvent with wide sources, excellent performance and multi-functional reagent, has been paid more and more attention by researchers.Based on this, by focusing on the cross-coupling reaction and free radical reaction, the application of DMSO/ DMSO-d6 as methylation/trideuterium methylating reagent in organic synthesis is systematically described, and the relevant reaction mechanism, development trend and challenges in the synthesis process are discussed.Keywords dimethyl sulfoxide (DMSO); DMSO-