18-Sep-21 News Discovery of (11bR)-4-Hydroxy-2,6-bis(2,4,6-triisopropylphenyl)dinaphtho[2,1-d:1′,2′-f][1,3,2]dioxaphosphepine 4-oxide

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Reference of 791616-63-2. Let’s face it, organic chemistry can seem difficult to learn. Especially from a beginner’s point of view. Like 791616-63-2, Name is (11bR)-4-Hydroxy-2,6-bis(2,4,6-triisopropylphenyl)dinaphtho[2,1-d:1′,2′-f][1,3,2]dioxaphosphepine 4-oxide. In a document type is Article, introducing its new discovery.

In this communication, we report the discovery of 1S (apremilast), a novel potent and orally active phosphodiesterase 4 (PDE4) and tumor necrosis factor-alpha inhibitor. The optimization of previously reported 3-(1,3-dioxo-1,3-dihydroisoindol-2-yl)-3-(3,4-dimethoxyphenyl)propionic acid PDE4 inhibitors led to this series of sulfone analogues. Evaluation of the structure-activity relationship of substitutions on the phthalimide group led to the discovery of an acetylamino analogue 1S, which is currently in clinical trials.

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Reference:
Chiral Catalysts,
Chiral catalysts – SlideShare