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Purpose
Typical Nutrient

Vitamins

The discovery and synthesis of vitamins 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 of vitamins, 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 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 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 amine-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 Verner McCollum 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 determine chemical structures, they resorted to an alphabetization scheme, naming the fat-soluble substance vitamin A and the water-soluble substance vitamin B. In 1920, a scurvy-curing substance was isolated and named vitamin C.

Through the 1920s, the pace of vitamin research and chemistry stepped up markedly, particularly in Europe's emerging drug industry. In 1927, Merck and Bayer teamed up to launch the first synthetic vitamin--a vitamin D product called Vigantol. In 1934, Merck followed with a vitamin C product called Cebion.

TO YOUR HEALTH Otto Isler (left) did pioneering work for Roche in the 1940s on the synthesis of vitamins A, E, and K. He is shown in his lab with his assistant Gody Ryser.DSM PHOTO

TO YOUR HEALTH Otto Isler (left) did pioneering work for Roche in the 1940s on the synthesis of vitamins A, E, and K. He is shown in his lab with his assistant Gody Ryser.

RESEARCHERS AT ROCHE, meanwhile, became interested in vitamins because of their physiological connections to hormones, which the company was extracting from animal organs and selling. According to a history of Roche published in 1996 for the company's 100th anniversary, the firm was set to enter the vitamin C market in the early 1930s using a technique developed by the Hungarian chemist Albert von Szent-Györgyi involving isolation of the vitamin from paprika.

In 1933, however, Tadeus Reichstein, a chemist at the Swiss Institute of Technology, offered Roche a four-step process for making vitamin C that used both microbial oxidation and chemical synthesis. Roche adopted the process and within a few years was producing thousands of kilograms of the vitamin every month. DSM 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-1--but Roche's process, developed by the English chemist Alexander R. Todd, gave the company the edge in the marketplace. By 1939, Roche was the world's leading supplier of vitamins B, C, and E.

Although vitamins were initially sold as stand-alone dietary supplements, multivitamins and food fortification quickly followed. Fortification of milk with vitamin D started in 1932, while supplementation of flour with B vitamins and iron began in the late 1930s. To supply these new uses, drugmakers such as Roche, Pfizer, and the Merck companies on both sides of the Atlantic built large-scale vitamin plants across Europe and the U.S.

The vitamin business continued to grow throughout the 1940s, '50s, and '60s, but production process patents expired over time, and competition intensified. At the companies that pioneered them, vitamins began to take a back seat, becoming cash cows to fund the more lucrative business of discovering and developing branded pharmaceuticals.

U.S. drug companies exited the bulk vitamins business in the 1980s and early 1990s. The Europeans held on longer, but Merck finally started pulling out of individual vitamin markets in 2000. Roche's sale to DSM put a cap on the era of big drugmakers as vitamin producers.—MICHAEL MCCOY

C&EN SPECIAL ISSUE

The Top Pharmaceuticals
That Changed The World
Vol. 83, Issue 25 (6/20/05)
Table Of Contents

Ascorbic Acid

Vitamins structure

Name

  • L-Ascorbic acid

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 largest volume vitamin, with annual global consumption of about 100 million kg.