Felix Hoffmann (21 January 1868 – 8 February 1946) was a German chemist notable for re-synthesizing diamorphine (independently from C.R. Alder Wright who synthesized it 23 years earlier), which was popularized under the Bayer trade name of "heroin". He is also credited with synthesizing aspirin, though whether he did this under his own initiative or under the instruction of Arthur Eichengrün is contested.
A chemist is a scientist trained in the study of chemistry. Chemists study the composition of matter and its properties. Chemists carefully describe the properties they study in terms of quantities, with detail on the level of molecules and their component atoms. Chemists carefully measure substance proportions, reaction rates, and other chemical properties. The word 'chemist' is also used to address Pharmacists in Commonwealth English.
Charles Romley Alder Wright FCS, FRS was an English lecturer in chemistry and physics researcher at St. Mary's Hospital Medical School in London, England. He was a founder of the Royal Institute of Chemistry.
Bayer AG is a German multinational pharmaceutical and life sciences company and one of the largest pharmaceutical companies in the world. Headquartered in Leverkusen, where its illuminated corporate logo, the Bayer cross, is a landmark, Bayer's areas of business include human and veterinary pharmaceuticals; consumer healthcare products; agricultural chemicals and biotechnology products; and high-value polymers. The company is a component of the Euro Stoxx 50 stock market index. Werner Baumann has been CEO since 2016.
Felix Hoffmann was born on 21 January 1868 in Ludwigsburg, Germany, the son of an industrialist. In 1889, he started studying chemistry at the Ludwig Maximilian University of Munich to study pharmacy and ended it in 1890 with the pharmaceutical state exam. 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".In 1894, he joined Bayer as a research chemist.
Ludwigsburg is a city in Baden-Württemberg, Germany, about 12 kilometres (7.5 mi) north of Stuttgart city centre, near the river Neckar. It is the largest and primary city of the Ludwigsburg district with about 88,000 inhabitants. It is situated within the Stuttgart Region, and the district is part of the administrative region (Regierungsbezirk) of Stuttgart.
Germany, officially the Federal Republic of Germany, is a country in Central and Western Europe, lying between the Baltic and North Seas to the north, and the Alps to the south. It borders Denmark to the north, Poland and the Czech Republic to the east, Austria and Switzerland to the south, France to the southwest, and Luxembourg, Belgium and the Netherlands to the west.
Ludwig Maximilian University of Munich is a public research university located in Munich, Germany.
On 10 August 1897 Hoffmann synthesized acetylsalicylic acid (ASA) while working at Bayer under Arthur Eichengrün. By combining salicylic acid with acetic acid, he succeeded in creating ASA in a chemically pure and stable form. The pharmacologist responsible for verifying these results was skeptical at first, yet once several large-scale studies to investigate the substance's efficacy and tolerability had been completed, it was found to be an analgesic, antipyretic and antiinflammatory substance. The company then worked to develop a cost-effective production process that would facilitate the promising active ingredient to be supplied as a pharmaceutical product. In 1899 it was marketed for the first time under the trade name "Aspirin", initially as a powder supplied in glass bottles.
Arthur Eichengrün was a German Jewish chemist, materials scientist, and inventor. He is known for developing the highly successful anti-gonorrhea drug Protargol, the standard treatment for 50 years until the adoption of antibiotics, and for his pioneering contributions in plastics: co-developing the first soluble cellulose acetate materials in 1903, called "Cellit", and creating processes for the manufacture of these materials which were influential in the development of injection moulding. During World War I his relatively non-inflammable synthetic cellulose acetate lacquers, marketed under the name "Cellon", were important in the aircraft industry. He contributed to photochemistry by inventing the first process for the production and development of cellulose acetate film, which he patented with Becker.
An analgesic or painkiller is any member of the group of drugs used to achieve analgesia, relief from pain.
Antipyretics are substances that reduce fever. Antipyretics cause the hypothalamus to override a prostaglandin-induced increase in temperature. The body then works to lower the temperature, which results in a reduction in fever.
He also synthesized diamorphine (heroin), previously achieved by Charles Romley Alder Wright.
Heroin, also known as diamorphine among other names, is an opioid most commonly used as a recreational drug for its euphoric effects. Medically it is used in several countries to relieve pain or in opioid replacement therapy. Heroin is typically injected, usually into a vein; however, it can also be smoked, snorted or inhaled. The onset of effects is usually rapid and lasts for a few hours.
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.
Hoffman was never married and died without issue on 8 February 1946 in Switzerland.
Hoffmann first claimed to be the "inventor" of aspirin (as opposed to just the synthesizer) in a footnote to a German encyclopedia published in 1934, saying that his father had complained about the bitter taste of sodium salicylate, the only drug then available to treat rheumatism. The large doses (6–8 grams) of sodium salicylate that were used to treat arthritis commonly irritated the stomach lining and caused patients considerable pain and irritation. He claimed that he began looking for a less acidic formation which led him to synthesize acetylsalicylic acid, a compound that shared the therapeutic properties of other salicylates but not the strong acidity that he believed caused stomach irritations.
An alternative credit for developing aspirin has also been offered. In 1949, ex-Bayer employee Arthur Eichengrün published a paper in which he claimed to have planned and directed Hoffman's synthesis of aspirin along with the synthesis of several related compounds. He also claimed to be responsible for aspirin's initial surreptitious clinical testing. Finally, he claimed that Hoffmann's role was restricted to the initial lab synthesis using his (Eichengrün's) process and nothing more.
The Eichengrün version was ignored by historians and chemists until 1999, when Walter Sneader of the Department of Pharmaceutical Sciences at the University of Strathclyde in Glasgow re-examined the case and came to the conclusion that indeed Eichengrün's account was convincing and correct and that Eichengrün deserved credit for the invention of aspirin.Bayer denied this in a press release, asserting that the invention of aspirin was due to Hoffmann.
In 2002, he was inducted into the US National Inventors Hall of Fame.
Aspirin, also known as acetylsalicylic acid (ASA), is a medication used to treat pain, fever, or inflammation. Specific inflammatory conditions which aspirin is used to treat include Kawasaki disease, pericarditis, and rheumatic fever. Aspirin given shortly after a heart attack decreases the risk of death. Aspirin is also used long-term to help prevent further heart attacks, ischaemic strokes, and blood clots in people at high risk. It may also decrease the risk of certain types of cancer, particularly colorectal cancer. For pain or fever, effects typically begin within 30 minutes. Aspirin is a nonsteroidal anti-inflammatory drug (NSAID) and works similarly to other NSAIDs but also suppresses the normal functioning of platelets.
Nonsteroidal anti-inflammatory drugs (NSAIDs) are a drug class that reduce pain, decrease fever, prevent blood clots and, in higher doses, decrease inflammation. Side effects depend on the specific drug, but largely include an increased risk of gastrointestinal ulcers and bleeds, heart attack and kidney disease.
Salicylic acid (from Latin salix, willow tree) is a lipophilic monohydroxybenzoic acid, a type of phenolic acid, and a beta hydroxy acid (BHA). It has the formula C7H6O3. This colorless crystalline organic acid is widely used in organic synthesis and functions as a plant hormone. It is derived from the metabolism of salicin. In addition to serving as an important active metabolite of aspirin (acetylsalicylic acid), which acts in part as a prodrug to salicylic acid, it is probably best known for its use as a key ingredient in topical anti-acne products. The salts and esters of salicylic acid are known as salicylates.
In organic chemistry, the Diels–Alder reaction is a chemical reaction between a conjugated diene and a substituted alkene, commonly termed the dienophile, to form a substituted cyclohexene derivative. It is the prototypical example of a pericyclic reaction with a concerted mechanism. More specifically, it is classified as a thermally-allowed [4+2] cycloaddition with Woodward–Hoffmann symbol [π4s + π2s]. It was first described by Otto Diels and Kurt Alder in 1928. For the discovery of this reaction, they were awarded the Nobel Prize in Chemistry in 1950. Through the simultaneous construction of two new carbon–carbon bonds, the Diels–Alder reaction provides a reliable way to form six-membered rings with good control over the regio- and stereochemical outcomes. Consequently, it has served as a powerful and widely applied tool for the introduction of chemical complexity in the synthesis of natural products and new materials. The underlying concept has also been applied to π-systems involving heteroatoms, such as carbonyls and imines, which furnish the corresponding heterocycles; this variant is known as the hetero-Diels–Alder reaction. The reaction has also been generalized to other ring sizes, although none of these generalizations have matched the formation of six-membered rings in terms of scope or versatility. Because of the negative values of ΔH° and ΔS° for a typical Diels–Alder reaction, the microscopic reverse of a Diels–Alder reactions becomes favorable at high temperatures, although this is of synthetic importance for only a limited range of Diels-Alder adducts, generally with some special structural features; this reverse reaction is known as the retro-Diels–Alder reaction.
Robert Burns Woodward was an American organic chemist. He is considered by many to be the preeminent organic chemist of the twentieth century, having made many key contributions to the subject, especially in the synthesis of complex natural products and the determination of their molecular structure. He also worked closely with Roald Hoffmann on theoretical studies of chemical reactions. He was awarded the Nobel Prize in Chemistry in 1965.
Quinoline is a heterocyclic aromatic organic compound with the chemical formula C9H7N. It is a colorless hygroscopic liquid with a strong odor. Aged samples, especially if exposed to light, become yellow and later brown. Quinoline is only slightly soluble in cold water but dissolves readily in hot water and most organic solvents. Quinoline itself has few applications, but many of its derivatives are useful in diverse applications. A prominent example is quinine, an alkaloid found in plants. 4-Hydroxy-2-alkylquinolines (HAQs) are involved in antibiotic resistance.
The year 1897 in science and technology involved some significant events, listed below.
Phytochemicals are chemical compounds produced by plants, generally to help them thrive or thwart competitors, predators, or pathogens. The name comes from Greek, Modern φυτόν (phyton), meaning 'plant'. Some phytochemicals have been used as poisons and others as traditional medicine.
A prodrug is a medication or compound that, after administration, is metabolized into a pharmacologically active drug. Inactive prodrugs are pharmacologically inactive medications that are metabolized into an active form within the body. Instead of administering a drug directly, a corresponding prodrug might be used instead to improve how a medicine is absorbed, distributed, metabolized,and excreted (ADME). Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects.
Heinrich Dreser was a German chemist responsible for the aspirin and heroin projects at Bayer AG. He was also a key figure in creating the widely used modern drug codeine.
Redoxon was the brand name of the first artificially synthesized ascorbic acid. Redoxon was first marketed to the general public by Hoffman-La Roche in 1934, making it the first mass-manufactured synthetic vitamin in history. The brand is now owned by German pharmaceutical company Bayer and is sold in many countries.
Kyriacos Costa Nicolaou is a Cypriot-American chemist known for his research in the area of natural products total synthesis. He is currently Harry C. and Olga K. Wiess Professor of Chemistry at Rice University, having previously held academic positions at The Scripps Research Institute/UC San Diego and the University of Pennsylvania.
George Rosenkranz is a pioneering Mexican scientist in the field of steroid chemistry, who used native Mexican plant sources as raw materials. He was born in Hungary, studied in Switzerland and emigrated to the Americas to escape the Nazis, eventually settling in Mexico.
Edward Stone (1702–1768) was a Church of England cleric who discovered the active ingredient of aspirin.
The history of aspirin begins with its synthesis and manufacture in 1899. Before that, salicylic acid had been used medicinally since antiquity. Medicines made from willow and other salicylate-rich plants appear in clay tablets from ancient Sumer as well as the Ebers Papyrus from ancient Egypt. Hippocrates referred to their use of salicylic tea to reduce fevers around 400 BC, and were part of the pharmacopoeia of Western medicine in classical antiquity and the Middle Ages. Willow bark extract became recognized for its specific effects on fever, pain and inflammation in the mid-eighteenth century. By the nineteenth century pharmacists were experimenting with and prescribing a variety of chemicals related to salicin, the active component of willow extract.
Ralph Franz Hirschmann was a German American chemist who led a team that was responsible for the first organic synthesis of an enzyme, a ribonuclease.
Marshall D. Gates Jr. (1915–2003) was an American chemist, holding the position of C.F. Houghton Professor of Chemistry at the University of Rochester. He was an organic chemist whose research was in the field of natural product synthesis. He is best known for publishing the first total synthesis of morphine in 1952.