Non-steroidal anti-inflammatory compounds

More recently, the acyl migration reaction has been studied for a range of non-steroidal anti-inflammatory compounds. For example, a detailed study has... 

Acupoint injection therapy (APIT) is a rather recently introduced treatment method that probably did not exist in the practice of TCM acupuncture. Saline, or injected medicines, such as non-steroidal anti-inflammatory compounds, analgesics or vitamins and herbal injections, are introduced into acupxmctune points. A case of death was reported to be associated with the use of acupoint injection for the treatment of lower back pain [43 ]. 

Pharmaceuticals and intermediates represent another important class of compounds. General classes of drugs that may well lend themselves to the IBC technology include the chiral non-steroidal anti-inflammatory profen drugs, norephedryns, and intermediates for a number of important drug classes including (i-blockers and racemic switch candidates. 

Pd/P(t-Bu)., in the presence of Cy2NMe, is an unusually mild and versatile catalyst for Heck reactions of aryl chlorides (Tables 1 and 2) (as well as for room-temperature reactions of aryl bromides).21 22 23 Example A, the coupling of chlorobenzene with butyl methacrylate, illustrates the application of this method to the stereoselective synthesis of a trisubstituted olefin a-methylcinnamic acid derivatives are an important family of compounds that possess biological activity (e.g., hypolipidemic24 and antibiotic25) and serve as intermediates in the synthesis of pharmaceuticals (e.g., Sulindac, a non-steroidal anti-inflammatory drug26). Example B, the coupling of 4-chlorobenzonitrile with styrene, demonstrates that Pd/P(t-Bu). can catalyze the Heck reaction of activated aryl chlorides at room temperature. 

The hydrocarboxylation of styrene (Scheme 5.12) and styrene derivatives results in the formation of arylpropionic acids. Members of the a-arylpropionic acid family are potent non-steroidal anti-inflammatory dmgs (Ibuprofen, Naproxen etc.), therefore a direct and simple route to such compounds is of considerable industrial interest. In fact, there are several patents describing the production of a-arylpropionic acids by hydroxycarbonylation [51,53] (several more listed in [52]). The carbonylation of styrene itself serves as a useful test reaction in order to learn the properties of new catalytic systems, such as activity, selectivity to acids, regioselectivity (1/b ratio) and enantioselectivity (e.e.) in the branched product. In aqueous or in aqueous/organic biphasic systems complexes of palladium were studied exclusively, and the results are summarized in Table 5.2. 

Older and still widely-used analgesic compounds can cause unacceptable side-effects. This is especially the case for the traditional non-steroidal anti-inflammatory drugs (NSAIDs) which are associated with serious gastrointestinal complications such as bleeding, lesions and ulcers. Every year it is estimated that 16,500 NSAID-related deaths occur in the US alone, with 75,000 patients hospitalized. 

An important example is the resolution of the enantiomers of naproxen. Naproxen is a member of a family of compounds known as Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) which are 2-aryl propionic acids. This class also includes ibuprofen, the painkiller developed by Boots and marketed as Nurofen. 

The aim of this work is to investigate the adsorption and desorption of a pharmaceutical compound, taken as representative of a complex chemical molecule, on activated carbon. Nimesulide is a non steroidal anti-inflammatory drug currently used in defeating respiratory tract infections. 

Dietary compounds are represented in a number of highly successful drugs such as lovastatin 31 and salicylic acid, the archetypal statin and non-steroid anti-inflammatory drugs, respectively. Lovastatin occurs in the red yeast of rice Monascus ruber),91 an ingredient of Eastern cuisine used to give a red colour to the Pekinese duck, while salicylic acid is ubiquitous in plants.92 Other important dietary drug candidates are curcumin 32 from turmeric and capsaicin from hot pepper 33,93 while traces of pharmaceutical benzodiazepines (including diazepam) occur in common edible plants such as potatoes and cherries.5... 

Over 30 billion tablets of non-steroidal anti-inflammatory drugs (NSAID) were dispensed in the United States in 2000 approximately 16% represent prescriptions for NSAIDs [1]. One in seven inhabitants of the North American ( 50 milhon) is hkely to be treated with an NSAID for a rheumatologic disorder in any given year [3]. In 2004 nearly 112 milhon prescriptions were written for NSAIDs of which almost half, 50+ milhon were for COX-2 inhibitors [3A]. These compounds enjoy a remarkable benefit/risk ratio when used in the treatment of acute self-limited pain syndromes. Unfortunately, when taken for prolonged periods of time, either by the elderly or individuals with certain co-morbid conditions, the frequency of adverse reactions rises dramaticaUy. 

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