The amide derived from 4-hydroxy-l-proline and 2,6-dimethylaniline is a powerful ligand for Cu-catalyzed coupling of (hetero)aryl halides with sulfinic acid salts, allowing the formation of a wide range of (hetero)aryl sulfones from the corresponding (hetero)aryl halides at considerably low catalytic loadings. The coupling of (hetero)aryl iodides and sodium methanesulfinate proceeds at room temperature with only 0.5 mol % CuI and ligand, representing the first example for Cu-catalyzed arylation at both low catalytic loading and room temperature.

A short and efficient synthesis of (S)-N-Boc-2,6-dimethyltyrosine utilizing palladium-catalyzed directed C-H functionalization is described. This represents the first general method for the ortho-dimethylation of tyrosine derivatives and offers a practical approach for preparing this synthetically important building block. Notably, throughout the reaction sequence no racemization occurs at the susceptible α-chiral centers.

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Simple and improved conditions have been found to carry out the Biginelli reaction for the synthesis of 3,4-dihydropyrimidin-2(1H)-one derivatives. This synthesis was performed using potassium hydrogen sulfate as the promoter in glycol solution. Compared with the classical Biginelli reaction conditions, this new method has the advantage of excellent yields (85-99%) and short reaction time (0.5-2 h).

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A series of 4¢-aryl-2,2¢:6¢,2¢¢-terpyridines have been prepared by the one-pot reaction of 2-acetylpyridine with aromatic aldehydes in the presence of ammonium acetate under microwave irradiation. This method has the advantages of shorter route, easier workup, shorter reaction time, higher yield and more environmentally friendly conditions, compared to the conventional ones.

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((2S,4R)‐4‐Hydroxy‐N‐(2‐methylnaphthalen‐1‐yl)pyrrolidine‐2‐carboxamide (HMNPC), an amide derived from 4‐hydroxy‐L‐proline and 2‐methyl naphthalen‐1‐amine, is a powerful ligand for Cu‐catalyzed coupling of (hetero)aryl halides with sulfinic acid salts, allowing for first time the metal‐catalyzed coupling of (hetero)aryl chlorides and NaSO2Me. A considerable number of (hetero)aryl chlorides worked well, providing the pharmaceutically important (hetero)aryl methylsulfones in good to excellent yields.