VITAMINS - C&EN Global Enterprise (ACS Publications)

Jun 20, 2005 - ... industry from one based on extracts and simple chemical compounds to one that was firmly rooted in complex synthetic organic chemis...
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NUTRIENT

VITAMINS

T

HE DISCOVERY AND SYNTHESIS

ofvitamins by U.S. and European chemists in the early years of the 20th century played an important role in transforming the pharmaceutical industry from one based on extracts and simple chemical compounds to one that was firmly rooted in complex synthetic organic chemistry Vitamins also played a big role in the rise of drug companies like Switzerland's F. Hoffmann-La Roche and Germany's E. Merck. In the course of supplying the essential nutrients to a population that often lacked them, these companies learned how to carry out pharmaceutical chemistry with efficiency and on an industrial scale. Today vitamins are a big business and vitamin deficiencies still plague the developing world. The manufacture ofvitamins, however, has lost much of its glamour. Roche, for years the world's largest vitamins producer, was the last major drug company making them when it sold its business to the chemical firm DSM three years ago. The idea that certain elements in food

ASCORBIC ACID Name: L-Ascorbic acid CAS Registry: 50-81-7 Other names: Vitamin C Introduced: Tadeus Reichstein, a chemist at the Swiss Institute of Technology, developed a practical synthesis of vitamin C in 1933 that is widely employed to this day. Sales: Today, vitamin C is the H0V OH largest volume vitamin, with HO^'Ar^O annual global OH consumption of about 100 million kg.

could be essential to health emerged in the seafaring era launched by Christopher Columbus. Doctors determined that sailors who came down with scurvy could easily be cured with citrus fruits, although they didn't understand why Beriberi, a disease prevalent in Asia, was found to be treatable by feeding patients whole-grain brown rice rather than white rice, which has its vitamin-rich husk removed. In 1912, the Polish chemist Casimir Funk was investigating beriberi by soaking 136

C & E N / J U N E 20, 2005

and most other vitamin producers continue to use the Reichstein process today Indeed, while Roche scientists were often not the first to discover vitamin syntheses, they typically came up with commercially advantageous processes. For example, in the mid-1930s, German and U.S. groups were the first to synthesize McCollum and Davis' vitamin B—by then known as vitamin B-l—but Roche's process, developed by the English chemist

brown rice in water and capturing the substance that dissolved. Funk determined that this substance contained an amine group. He went on to posit the existence of a whole range of amme-containing substances that were vital for good health, naming them vitamines. The "e" was dropped later when scientists realized that not all of these substances were amines. In 1913, two American chemists, Elmer VernerMcCollum and Marguerite Davis, found something in butter and egg yolks that, when removed from the diets of rats, caused night blindness. McCollum and Davis knew that this fat-soluble substance could not be the same one found in brown rice. Lacking the know-how TO Y O U R H E A L T H Otto Isler (left) did pioneering to determine chemical struc- work for Roche in the 1940s on the synthesis of tures, they resorted to an al- vitamins A, Ep and K. He is shown in his lab with his phabetization scheme, nam- assistant Gody Ryser. ing the fat-soluble substance vitamin A and the water-soluble substance Alexander R. Todd, gave the company the vitamin B. In 1920, a scurvy-curing subedge in the marketplace. By 1939, Roche stance was isolated and named vitamin C. was the world's leading supplier of vitamins B, C, and E. Through the 1920s, the pace of vitamin Although vitamins were initially sold as research and chemistry stepped up markstand-alone dietary supplements, multiviedly particularly in Europe's emerging drug tamins and food fortification quickly folindustry In 1927, Merck and Bayer teamed lowed. Fortification of milk with vitamin up to launch the first synthetic vitamin— D started in 1932, while supplementation a vitamin D product called Vigantol. In of flour with Β vitamins and iron began in 1934, Merck followed with a vitamin C the late 1930s. To supply these new uses, product called Cebion. drugmakers such as Roche, Pfizer, and the Merck companies on both sides of the At­ RESEARCHERS AT ROCHE, meanwhile, lantic built large-scale vitamin plants across became interested in vitamins because of Europe and the U.S. their physiological connections to horThe vitamin business continued to grow mones, which the company was extractthroughout the 1940s, '50s, and '60s, but ing from animal organs and selling. Acproduction process patents expired over cording to a history of Roche published in time, and competition intensified. At the 1996 for the company's 100th anniversary, companies that pioneered them, vitamins the firm was set to enter the vitamin C began to take a back seat, becoming cash market in the early 1930s using a technique cows to fund the more lucrative business developed by the Hungarian chemist Alof discovering and developing branded bert von Szent-Gyôrgyi involving isolation pharmaceuticals. of the vitamin from paprika. U.S. drug companies exited the bulk vi­ In 1933, however, Tadeus Reichstein, a tamins business in the 1980s and early chemist at the Swiss Institute of Technol1990s. The Europeans held on longer, but ogy, offered Roche a four-step process for Merck finally started pulling out of indi­ making vitamin C that used both microvidual vitamin markets in 2000. Roche's bial oxidation and chemical synthesis. sale to DSM put a cap on the era ofbig drugRoche adopted the process and within a makers as vitamin producers.—MICHAEL fewyears was producing thousands of kiloMCCOY grams of the vitamin every month. DSM WWW.CEN-0NLINE.ORG