1042722-98-4

Upstream product

• 596-43-0 bromo-triphenyl-methane 
• 191330-56-0 [14C]-Sch 57871 
• 1042723-13-6 3-{(3R,4S)-1-(4-fluorophenyl)-2-oxo-4-[4-(trityloxy)phenyl]azetidin-3-yl}propionyl chloride 
• 352-13-6 4-flourophenylmagnesium bromide 

Downstream Products

• 1042722-68-8 C₄₃H₃₅F₂NO₃ 

Relevant academic research and scientific papers

A METHOD OF MANUFACTURING (3R,4S)-L-(4-FLUOROPHENYL)-3-[(3S)-3-(4-FLUOROPHENYL)-3- HYDROXYPROPYL)]-4-(4-HYDROXYPHENYL)-2-AZETIDINONE AND ITS INTERMEDIATES

A method of manufacturing (3R,4S)-l-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3- hydroxypropyl)]-4-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) of formula I, in which a protected ketone of general formula II, wherein R stands for a protective group, such as benzyloxycarbonyl, tert-butoxycarbonyl, benzhydryl or trityl, is reduced with asymmetrical borane agents in an inert organic solvent in the temperature range of -30 to +40 °C, and finally the obtained protected alcohol of general formula III, wherein R has the same meaning as above, is deprotected by the action of hydro genolytic or acidic agents in an inert organic solvent.

Process for the preparation of ezetimibe and derivatives thereof

The present invention relates to the method of preparing of ezetimibe and in particular to novel intermediates for its synthesis and an improved process for preparing such intermediates. Said intermediates may be obtained in high yields and purity in a fast and cost efficient manner. The present invention relates to a novel crystalline form of ezetimibe as well.