Sternbach, Leo

The benzodiazepines were discovered by Leo Sternbach at the Hoffman-La Roche laboratories, and their pharmacology was elucidated by Randall of the same company. An enormous variety of these compounds exist. Since about 3500 benzodiazepine compounds have been investigated, the neurologic structure-activity relationships of these drugs have been well established and the central features can be generalized as follows ... 

Leo H. Sternbach was born in Austria in 1908. In 1918, after World War I and the dissolution of the Austro-Hungarian Empire,... 

The thinking that led to the discovery and exploitation of the benzodiazepines by Dr Leo Sternbach and his associates illustrates the way this was done. Any molecular scaffold they decided to work on would be expected to fulfill the following criteria (1) be relatively unexplored, (2) be readily accessible, (3) give the possibility of a multitude of variations and transformations, (4) offer some challenging chemical problems, and (5) look as if it could lead to biologically active products. " While the rate of compound synthesis in those days... 

THE DRUG SHOWN HERE IS DIAZEPAM, better known as Valium. It is commonly prescribed for a wide range of disorders, including anxiety, insomnia, seizures, muscle spasms, restless legs syndrome, and obsessive-compulsive disorder. Valium was invented by Leo Sternbach at Hoffmann-LaRoche Pharmaceuticals and first licensed for use in 1960. 

In 1946, Moses W. Goldberg (1905-1964) and Leo H. Sternbach from Hoffmann-La Roche filed the first of several patent applications relating to the synthesis of biotin (Fig. 7.48). The starting material was fumaric acid, which was tra/is-dibrominated. NucleophEic substitution with benzylamine, cyclisation with phosgene and treatment with acetic anhydride gave the cis-substituted meso-imidazolidinone, which was converted with cydohexanol into the halfester. The enantiomers were then separated with (-)-ephedrine. Alternatively,... 

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