937798-07-7

Upstream product

• 99395-88-7 (S)-4-phenyl-2-oxazolidinone 
• 189028-93-1 (S)-1-(4-fluorophenyl)-5-(2-oxo-4-phenyloxazolidin-3-yl)pentane-1,5-dione 
• 18162-48-6 tert-butyldimethylsilyl chloride 
• 189028-95-3 (4S)-3-[(5S)-5-(4-fluorophenyl)-5-hydroxypentanoyl]-4-phenyl-1,3-oxazolidine-2-one 
• 462-06-6 fluorobenzene 
• 108-55-4 glutaric anhydride, 
• 189028-94-2 (S)-5-(4-fluorophenyl)-5-hydroxypentanoic acid 

Downstream Products

• 937798-06-6 3-[2-[(2-benzyloxy-4-benzyloxymethylphenyl)-(4-fluorophenylamino)methyl]-5-(tert-butyldimethylsilanyloxy)-5-(4-fluorophenyl)pentanoyl]-4-phenyloxazolidin-2-one 
• 1023328-36-0 tert-butyl 4-[(1S,2R,5S)-5-(tert-butyldimethylsilanyloxy)-5-(4-fluorophenyl)-1-(4-fluorophenylamino)-2-((S)-4-phenyloxazolidin-2-one-3-carbonyl)pentyl]-3-fluorophenyl piperazine-1,4-dicarboxylate 
• 1023328-39-3 (S)-3-[(S)-2-[(4-benzyloxy-2-fluorophenyl)(4-fluorophenylamino)methyl]-5-(tert-butyldimethylsilanyloxy)-5-(4-fluorophenyl)pentanoyl]-4-phenyloxazolidin-2-one 
• 163222-33-1 ezetemibe 

Relevant academic research and scientific papers

Iridium-Catalyzed Asymmetric Hydrogenation of ?- A nd ?-Ketoacids for Enantioselective Synthesis of ?- A nd ?-Lactones

A highly efficient asymmetric hydrogenation of ?- A nd ?-ketoacids was developed by using a chiral spiro iridium catalyst (S)-1a, affording the optically active ?- A nd ?-hydroxy acids/lactones in high yields with excellent enantioselectivities (up to >99% ee) and turnover numbers (TON up to 100000). This protocol provides an efficient and practical method for enantioselective synthesis of Ezetimibe.

Novel ezetimibe derivative and preparation method thereof

The invention provides a novel ezetimibe derivative. The structural formula of the novel ezetimibe derivative is as shown in specification. By the ezetimibe derivative, the water solubility of ezetimibe is improved, and clinical application of drugs is facilitated.

according to folds Mai Bu and its intermediate synthesis method

The invention provides an Ezetimibe synthesis method comprising the following steps: (a) a compound (5) is subjected to asymmetric reduction reaction to obtain a compound (6), and the compound (6) and tert-butyldimethylsilyl chloride react in an organic solution under the action of alkali to obtain a compound (7); (b) the compound (7) and diisopropylethylamine are dissolved in the organic solution, titanium tetrachloride is added in the organic solution to react at 20-50 DEG C, and a compound (3) is added in the organic solution at minus 20 to minus 60 DEG C to react to obtain a compound (8); (c) the compound (8) and N,O-bis(trimethylsilyl) acetamide react in the organic solution at 20-80 DEG C, tetrabutylammonium fluoride trihydrate is added into the organic solution to react at 20-80 DEG C to obtain a compound (9); (d) the compound (9) is subjected to off-protection reaction to obtain Ezetimibe, wherein R is equal to TBS, Ac or COOCH2CCl3. The invention further provides an Ezetimibe intermediate and a preparation method thereof.