Felix Hoffmann and the Synthesis of Aspirin

Felix Hoffman

Felix Hoffman (1868-1946)

On August 10, 1897German chemist Felix Hoffmann  synthesized acetylsalicylic acid (ASA) in a stable form usable for medical applications. In 1899 it was marketed for the first time under the trade name Aspirin. Acetylsalicylic acid, the active ingredient of aspirin, was first discovered from the bark of the willow tree in 1763 by Edward Stone of Wadham College, University of Oxford.

Felix Hoffmann was born on January 21, 1868 and grew up in Swabia, Germany. He was employed in various pharmacies across the country and also studied chemistry and pharmacy at the University of Munich. In 1891 he graduated magna cum laude from the University of Munich. Two years later he earned his doctorate, also magna cum laude, after completing his thesis entitled “On certain derivatives of dihydroanthracene“. Adolf von Baeyer recommended the young man to join the pharmeceutical research department at the Bayer Company in Elbersfeld as a research chemist.

In 1897, Hoffmann added the acetyl group to various molecules hoping one the one hand to decrease the toxicity and on the other to improving the strength of physiologically active substances while working at Bayer under Arthur Eichengrün. There is a legend which says that Hoffmann searched for a medicine against his father’s rheumatic pains. The pain releaving properties of willow bark were known for a long time and in 1859, Hermann Kolbe managed to synthesize it. In the 1870s, it was first sold, but its side effects (e.g. stomach pain) were often too much for the patients to handle. When Hoffmann acetylated salicylic acid to produce acetylsalicylic acid, Heinrich Dreser tested the substance on patients in a hospital in Halle, Germany. It was named Aspirin, ‘A’ for acetyl and ‘spirin’ from Spirea, the genus name for shrubs that are an alternative source of salicylic acid. Unfortunately, the sources on the origins of Aspirin differ. Evidence has surfaced that Arthur Eichengrün played a more significant role as admitted by Bayer and it is possible that he was left out in the story (which has been told approximately since the 1930s) because Eichengrün was Jewish. Arthur Eichengrün claimed to be the inventor of aspririn after World War II and in later years, it was found that many of Eichengrün’s arguments were convincing. However, Bayer always denied this and asserted that the invention of aspirin was due to Hoffmann. When Bayer applied for a patent, it turned out that acetylsalicylic acid had been synthesized earlier, even though it was probably not as pure as Hoffmann’s.

However, Felix Hoffmann not only succesfully synthesized acetylsalicylic acid in a stable form usable for medical applications and thus, creating one of the most widely beneficial drugs of all time. In a two-week period, Hoffmann also synthesized heroin, one of the most harmful drugs. He was asked by Dreser to acetylate morphine in order to produce codeine, but created heroin. The compound had already been discovered in 1874 and could not be patented. Before the high risk of addiction using heroin was discovered, the drug was sold by Bayer to cure coughs, to relieve pain in extreme situations like childbirth, and to control various mental disorders.

Following the synthesis of aspirin, Hoffmann moved to the pharmaceutical marketing department where he stayed until his retirement in 1928. He was granted full power of attorney over Aspirin.

On February 8, 1946 Felix Hoffmann died retired and without descendants in Switzerland.

At yovisto academic video search, you may enjoy a TED talk by James Leitzel on the legalization of drugs.

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