One kind in accordance with the preparation method of the folds Mai Bu key intermediate
The invention relates to an improvement of a method for preparing a key ezetimibe intermediate (S)-3-{(R)-2-(S)-4-benzyloxyphenyl-[4-fluorophenylamido-methyl]-4-[2-(4-fluorophenyl)-[1,3]dioxolane -2-yl]-butyryl}-4-phenyl-oxazolidinyl-2-one (V). A target product ezetimibe can be obtained through carrying out a nine-step reaction on a raw material glutaric anhydride by applying the improved method. Compared with previous methods, the ezetimibe preparation method of the invention has the advantages of reaction step shortening, operation simplifying, and product yield improving, and solves a problem that the industrialized production of ezetimibe is difficult.
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Paragraph 0011; 0021-0023
(2017/04/25)
PROCESSES FOR PREPARING INTERMEDIATE COMPOUNDS USEFUL FOR THE PREPARATION OF EZETIMIBE
The invention relates, in general, to an improved process for the preparation of the compounds (3R,4S)-4-(4-(benzyloxy)phenyl)-1-(4-fluorophenyl)-3-[3-(4-fluorophenyl)-3-oxopropyl]azetidin-2-one and (3R,4S)-1-(4-fluorophenyl)-3-[3-(4-fluorophenyl)-3-oxopropyl]-4-(4-hydroxyphenyl)-azetidin-2-one, which are key intermediates for the synthesis of ezetimibe, as well as the use of these intermediates for the preparation of ezetimibe.
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Page/Page column 15
(2009/09/26)
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