956368-72-2

Upstream product

• 1056209-19-8 methyl 2-[(2R)-2-[tert-butyl(dimethyl)silyl]oxy-2-(4-fluorophenyl)ethyl]thioacetate 
• 403-29-2 2-bromo-4'-fluoroacetophenone 
• 1369489-38-2 methyl 2-[(2R)-2-(4-fluorophenyl)-2-hydroxyethyl]thioacetate 
• 18162-48-6 tert-butyldimethylsilyl chloride 
• 1097211-38-5 (1R)-2-bromo-1-(4-fluorophenyl)ethan-1-ol 
• 1056209-16-5 (1R)-2-bromo-1-(t-butyldimethylsilyloxy)-1-(4-fluorophenyl)ethane 

Downstream Products

• 956368-62-0 methyl {4-[(2R,3R)-3-{[(2R)-2-{[tert-butyl(dimethyl)silyl]oxy}-2-(4-fluorophenyl)ethyl]thio}-1-(4-iodophenyl)-4-oxoazetidin-2-yl]phenoxy}acetate 
• 1056209-21-2 (4S)-3-{2-[(2R)-2-(4-fluorophenyl)-2-(1,1,2,2-tetramethyl-1-silapropoxy)ethylthio]acetyl}-4-phenyl-1,3-oxazolidin-2-one 
• 1369489-40-6 C₁₀H₁₇N*C₂₅H₂₁F₂NO₅S 

Relevant academic research and scientific papers

Selection and development of a route for cholesterol absorption inhibitor AZD4121

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.

1-BIARYLAZETIDINONE DERIVATIVES

The object of the present invention is to provide a compound having an excellent cholesterol-lowering effect and to provide a drug for the treatment, prevention of onset, or prevention of progress of lipid metabolism disorder, hyperlipidemia, or atheroscl

BIPHENYLAZETIDINONE CHOLESTEROL ABSORPTION INHIBITORS

The invention relates to a chemical genus of 4-biphenyl-1-phenylazetidin-2-ones useful in the treatment of hypercholesterolemia and other disorders. The compounds have the general formula (I). Pharmaceutical compositions and methods for treating cholesterol- and lipid-associated diseases are also disclosed.