56841-99-7Relevant academic research and scientific papers
Synthetic method of apremilast intermediate
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Paragraph 0018; 0037-0038, (2021/04/26)
The invention discloses a synthetic method of an apremilast intermediate. The method comprises the following steps of by taking 2-methoxyphenyl acetate and 2-(methylsulfonyl) acetyl chloride as starting materials, carrying out acylation reaction and hydrolysis under the catalysis of aluminum trichloride to obtain 1-(3-hydroxy-4-methoxyphenyl)-2-(methylsulfonyl) ethyl ketone, carrying out alkylation reaction with bromoethane, and then forming imine with ammonium acetate, and reducing to form the 1-(3-ethoxy-4-methoxy phenyl)-2-(methylsulfonyl) ethylamine. The method is simple to operate, avoids the use of n-butyllithium, palladium on carbon and mesylate, avoids the problems of high risk, high cost and the like, and is suitable for industrial production.
Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma
Onions, Stuart T.,Ito, Kazuhiro,Charron, Catherine E.,Brown, Richard J.,Colucci, Marie,Frickel, Fritz,Hardy, George,Joly, Kevin,King-Underwood, John,Kizawa, Yasuo,Knowles, Ian,Murray, P. John,Novak, Andrew,Rani, Anjna,Rapeport, Garth,Smith, Alun,Strong, Peter,Taddei, David M.,Williams, Jonathan G.
, p. 1727 - 1746 (2016/03/25)
The discovery of a novel series of therapeutic agents that has been designed and optimized for treating chronic obstructive pulmonary disease is reported. The pharmacological strategy was based on the identification of compounds that inhibit a defined subset of kinase enzymes modulating inflammatory processes that would be effective against steroid refractory disease and exhibit a sustained duration of action after inhaled delivery.
