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Updated: Oct 11, 2026

Synthesis of a Borylated Ibuprofen Derivative Through Suzuki Cross-Coupling and Alkene Boracarboxylation Reactions
Published on: November 30, 2022
[Rofecoxib, a new NSAID preparation with selective COX-2 inhibition]
1Medicinsk afdeling E, Amtssygehuset i Herlev.
Abstract:
NSAIDs are effective by inhibition of the enzyme cyclooxygenase, which leads to formation of prostaglandins. At the beginning of the 90-ties it became evident, that cyclooxygenase existed in two isoforms (COX-1 and COX-2). COX-1 is found in a number of tissues. In these tissues prostaglandins have several physiological functions. COX-2 is an induceable enzyme involved in inflammation. A new NSAID, rofecoxib, has selective COX-2 inhibition defined as inhibition of COX-2, but not COX-1 in the therapeutic dose range. Trial results have shown pain relief analogous to common NSAIDs (ibuprofen and diclofenac) in patients with osteoarthritis of the hip or knee. The incidence of gastric ulcers was significantly reduced in the rofecoxib treated group compared to the groups treated with common NSAIDs. It is concluded that selective COX-2 inhibition is a promising new treatment. At present it seems appropriate to consider the drug in patients with good indication for an NSAID and simultaneous gastrointestinal risk factors.
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