Boots Company

Other Formulations. In addition to those described above, systems have been reported for parenterals [25], film coatings [26], and topicals [27], All use the Formulogic shell, the last one winning a prize for the Boots Company in 1991. All contain elements of the features of systems discussed above. 

Bronopol (Myacide AS) is a potent antibacterial agent with some activity against yeasts. It was developed originally by the Boots Company in the UK as a preservative for cosmetics and toiletry products and has been used extensively in these areas since the 1970s. More recently it has been adopted in industrial formulation systems due to its low use concentrations and good compatibility... 

A classic example of improving the route to a commercial product is ibuprofen (1.16), which is an analgesic (a pain reliever) and is also effective as a non-steroidal antiinflammatory drug. Ibuprofen was produced using six steps (Scheme 1.8) by the Boots Company, with an overall atom economy of just 40%. 

In the 1990s the Hoechst Celanese Corporation (together with the Boots company they formed the BHC process to prepare and market ibuprofen, 1.16) developed a new three-stage process (Scheme 1.9), with an atom economy of 77.4%. 

In the early 1970s the area of carbamoyl heterocycles had been a fruitful area of synthesis for organic chemists working in the Boots Company in Nottingham, yielding for example, the herbicide epronaz (I) (1) as well as compounds active in other fields. 

Around this time Tolkmith and his colleagues (2) drew attention to the fungicidal activity of the thiocarboxamide (II) and this acted as a spur for workers at the Boots Company to undertake further... 

The purpose of this paper is to review various aspects of the work done in the prochloraz area in the laboratories of the Boots Company, and latterly (following ownership changes) in the laboratories of FBC Ltd and by the agrochemical division of Schering AG West Germany. The review will describe the synthesis of the various types of compound prepared as the project evolved, and will consider their mode of action and the usefulness of an in vitro assay as a guide to synthesis. It will also deal briefly with the biological activity of prochloraz itself. Some of this information has already been published (4). 

I am Indebted to many colleagues who have worked on this project over a number of years, and without whose contribution this review could not have been written. In particular, I would like to acknowledge the Inventive contributions of R.F.Brookes, D.H.Godson, A.F.Hams, D.M.Weighton and W.H.Wells who were employed at the Boots Company. 

Webster Systems (now taken over by the Boots Company)... 

Of the 1-carbamoyl imidazole derivatives The Boots Company found the compounds BTS 40 542 to be the most potent fungicide (Birchmore et al., 1977). The scheme of preparation of prochloraz is the following (Brookes et al.. 1973) ... 

Ibuprofen was developed by researchers at the Boots Company, a British drug manufacturer, in the early 1960s. Those researchers had found that the anti-inflammatory property of aspirin was due to the presence of a carboxylic acid (-COOH) group in the compound. They searched for other carboxylic acids that might have similar properties and, after testing more than 600 compounds, discovered that ibuprofen met that criterion. It was twice as effective as... 

Early 1960s Ibuprofen is developed by researchers at the Boots Company, a British drug manufacturer. 

This Is an issue where consensus now seems to have been achieved. An ingenious theorem due to Fieller (Fieller, 1940, 1944) enables one to calculate a confidence interval for the ratio of two means. The approach does not require transformation of the original data. (Edgar C. Fieller, 1907—1960, is an early example of a statistician employed in the pharmaceutical industry. He worked for the Boots company in the late 1930s and 1940s.) For many years this was a common approach to making inferences about the ratio of the two mean AUCs in the standard bioequivalence experiment (Locke, 1984). 

Stewart Adams and John Nicholson at the Boots Company in Nottingham took acetylsalicylic acid as a lead template and looked for related anti-inflammatory structures, which would be devoid of the ASA-related side-effect. In 1955, they discovered that their anti-inflammatory compounds reduced skinreddening (erythema) in guinea-pigs, caused by ultraviolet irradiation. Thereby they had foimd a simple and feasible assay system to test a whole host of compounds. In 1961, out of a group of several hundred substances they were able to select the one, which was introduced to the British market in 1969 under the name ofibuprofen (Fig. 5.83). [180]... 

In the 1980s the Boots company developed the serotonin- and norepinephrine-reuptake inhibitor sibutramine for reduction of severe overweight. [242, 244] Sibutramine has a dual function to increase the feeling of satiety and to enhance metabolism. In 1997, the drug was launched under the trade name Meridia , however after an unfavourable risk/benefit assessment and the consequent ban by the European Medicines Agency (EM A) and the FDA, it was ultimately suspended by Abbott in 2010. 

Sir Jack Cecil Drummond was a distinguished British biochemist, noted for his scientific work on nutrition during the Second World War. In 1944, he was elected Fellow of the Royal Society and knighted in the same year. After the war, he became Director of Research at the Boots Company in Nottingham. 

Haslam, M. The Chilwell Story VC Factory and Ordnance Depot (Nottingham The Boots Company, 1982). 

Lankro Ltd (now Harcros Chemicals) Rhone-Poulenc Industrialisation, France BASF Chemicals Ltd Burgoyne Consultants Ltd Boots Company pic... 

Guthrie WG (1984) Analysis of bronopol in water-based lotion. Provisional HPLC method. The Boots Company PLC, Nottingham... 

The BHC Company is a joint venture of the Hoechst Celanese Corporation and the Boots Company. BASF purchased the Boots Company and Celanese sold its interest in the BHC Company to BASF. Celanese operates the new ibuprofen manufacturing facility in Bishop, Texas, for BASF. Ibuprofen manufactured via the BHC process is marketed under the brand names Advil and Motrin. The industrial-scale facility created in Bishop, Texas, in 1992 is the world s largest ibuprofen manufacturing plant, is operated by the Celanese Corporation for BASF, and currently produces approximately 20-25 % (more than 7 million pounds) of the world s yearly supply of ibuprofen. 

Ibuprofen, a widely used over-the-counter analgesic, is made by the classical route developed by the Boots Company as shown below. This process involves six step-wise reactions, including Friedel-Crafts acylation on the first step. Such a process entails too many synthetic steps, thus decreasing the overall yields, and also generating substantial amounts of waste by-products, such as inorganic salts. 

The traditional commercial synthesis of ibuprofen was developed by the Boots Company of England in 1960s (U.S. Patent 3,385,886). This synthesis is given (Scheme 22). 

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