Category: esters-buliding-blocks. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: (11bR)-N,N-Bis[(1R)-1-phenylethyl]dinaphtho[2,1-d:1′,2′-f][1,3,2]dioxaphosphepin-4-amine, is researched, Molecular C36H30NO2P, CAS is 415918-91-1, about Methyl-monofluorination of ibuprofen selectively increases its inhibitory activity toward cyclooxygenase-1 leading to enhanced analgesic activity and reduced gastric damage in vivo. Author is Su, Hong; Xie, Yuli; Liu, Wen-Bo; You, Shu-Li.
Newly developed monofluoromethylation reaction provided access to various bioactive mols. with an interesting monofluoromethyl unit. An iridium-catalyzed asym. version was employed for large-scale methyl-monofluorination of widely used nonsteroidal anti-inflammatory drug ibuprofen (the active S isoform). The methyl-monofluorinated ibuprofen was found to selectively inhibit cyclooxygenase-1 over cyclooxygenase-2 and surprisingly, the compound, with almost equal pharmacokinetic profile, was shown to increase analgesic activity and diminish gastric damage in animal models comparing to the parent drug ibuprofen. Therefore, methyl-monofluorination could be a useful strategy for improving efficacy and safety profile of drugs from the ‘profen’ family.
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Reference:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics