1450876-94-4

Upstream product

• 446292-07-5 2-((2S)-2-hydroxy-3-{[4-(3-oxomorpholin-4-yl)phenyl]amino}propyl)-1H-isoindole-1,3(2H)-dione 
• 530-62-1 1,1'-carbonyldiimidazole 

Downstream Products

• 446292-08-6 2-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-1H-isoindole-1,3(2H)-dione 

Relevant academic research and scientific papers

A PROCESS FOR THE PREPARATION OF RIVAROXABAN BASED ON SAVING OF 1,1'-CARBONYL DIIMIDAZOLE.

The invention provides a method of carrying out the cyclization of the compound of formula (14) to the compound (15), wherein first a non-cyclic intermediate (16) is prepared by the treatment with 1 to 1.5 equivalents of 1,1'-carbonyldiimidazole of formula (8), which further converts into the cyclic product (15) by treatment with heat or a base. The present method of cyclization of the compound (14) to the compound (15) is preferred and distinguished from the prior methods by the use of a lower amount of the expensive carbonylation agent, which is compensated by use of a cheap base (17), wherein R means an alkyl and M means an alkali metal.