发明名称 A PROCESS FOR THE PREPARATION OF RIVAROXABAN BASED ON SAVING OF 1,1'-CARBONYL DIIMIDAZOLE.
摘要 <p>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.</p>
申请公布号 WO2013120464(A1) 申请公布日期 2013.08.22
申请号 WO2013CZ00014 申请日期 2013.02.12
申请人 ZENTIVA, K.S. 发明人 HALAMA, ALES;KRULIS, RADIM;BRICHAC, JIRI
分类号 C07D409/14 主分类号 C07D409/14
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