Practical Synthesis of β‐Carbonyl Phenyltetrazolesulfones and Investigations of Their Reactivities in Organocatalysis

A practical synthesis of β‐carbonyl phenyltetrazolesulfones, useful for a series of enantioselective reactions, is shown. Aryl, alkyl and ester carbonyl compounds all proved to be efficiently synthesised, leading to products in up to >99 % yield over two steps. During this procedure, no special attention to conditions or laborious purification by chromatography is needed. Furthermore, X‐ray crystallography, kinetic studies, as well as NMR and IR investigations provide insights into the reactivities of these compounds in organocatalysis.