917577-70-9Relevant academic research and scientific papers
Selection and development of a route for cholesterol absorption inhibitor AZD4121
Karlsson, Staffan,Soerensen, J. Henrik
experimental part, p. 586 - 594 (2012/07/03)
The development of a synthetic route to the cholesterol absorption inhibitor AZD4121 is presented. Key steps are a highly enantioselective CBS reduction, a stereospecific Staudinger reaction, an amine/lithium chloride mediated ester hydrolysis, and a resolution of a 50:50 diastereomeric mixture by recrystallization. The synthesis was accomplished in 10 linear steps, and the overall yield, when compared with the lead optimization (LO) route, was improved from 1% to 20%. All purifications of intermediates through preparative HPLC or silica gel chromatography were avoided. This was possible since many of the intermediates along the route could be used as such in the next step until an intermediate with suitable crystalline properties could be identified and purified through crystallization.
NEW 2-AZETIDINONE DERIVATIVES USEFUL IN THE TREATMENT OF HYPERLIPIDAEMIC CONDITIONS
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Page/Page column 63, (2010/11/25)
The invention relates to compounds of formula (I) and pharmaceutically acceptable salts, solvates, and prodrugs thereof, and to their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia. The invention also relates to processes fo
NEW 2-AZETIDINONE DERIVATIVES AS CHOLESTEROL ABSORPTION INHIBITORS FOR THE TREATMENT OF HYPERLIPIDAEMIC CONDITIONS
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Page/Page column 62, (2010/11/25)
The invention relates to 2-azetidinone derivatives of formula (I) , including pharmaceutically acceptable salts, solvates and prodrugs thereof. The compounds inhibit cholesterol absorption and are useful in the treatment of hyperlipidaemic conditions. The
