Transition‐Metal‐Catalyzed Utilization of Methanol as a C1 Source in Organic Synthesis

Methanol is used as a common solvent, cost‐effective reagent, and sustainable feedstock for value‐added chemicals, pharmaceuticals, and materials. Among the various applications, the utilization of methanol as a C1 source for the formation of carbon–carbon, carbon–nitrogen, and carbon–oxygen bonds continues to be important in organic synthesis and drug discovery. In particular, the synthesis of C‐, N‐, and O‐methylated products is of central interest because these motifs are found in a large number of natural products as well as fine and bulk chemicals. In this Minireview, we summarize the utilization of methanol as a C1 source in methylation, methoxylation, formylation, methoxycarbonylation, and oxidative methyl ester formation reactions. Sustainable C1 source: Methanol serves as a sustainable feedstock for value‐added chemicals, materials, and life science molecules. It has also been used as a C1 source in methylation, methoxylation, formylation, methoxycarbonylation, and oxidative methyl ester formation reactions for the synthesis of C‐methylated products, N‐methylamines, formamides, urea derivatives, ethers, esters, and heterocycles.