Abstract
A short review is given of the basic chemical development in the field of ‘classical’ and ‘annelated’ benzodiazepines, distinguishing between pro‐drugs and directly acting compounds. Some properties of midazolam that are of special interest for its practical use are discussed, such as: the basicity of its imidazole ring nitrogen, which allows water‐ soluble salts and well‐tolerated aqueous injectable solutions to be prepared; its stability to hydrolytic degradation; its rapid metabolic inactivation, which is mainly determined by the methyl group on the imidazole ring, and which is much faster than that of classical benzodiazepines.