CAS: 156925-25-6; 4-Amino-5-Chloro-2-Ethoxy-N-((4-(4-Fluorobenzyl)Morpholin-2-yl)Methyl)Benzamide 2-Hydroxypropane-1,2,3-Tricarboxylate Dihydrate

上下游产品

mosapride (RS)-4-amino-5-chloro-2-ethoxy-N-{[4-(4-fluoro-benzyl)-2-morpholinyl]-methyl}-benzamide trifluoroacetate citric acid sodium p-aminosalicylate

专利信息

专利号:WO-03106440-A3
优先权日:2002-06-13
标题 :PROCESS FOR THE SYNTHESIS OF A BENZAMIDE DERIVATIVE
发明人：VUKICS KRISZTINA; FISCHER JANOS; LEVAI SANDOR; ERDELYI PETER
权利人:RICHTER GEDEON VEGYESZET; VUKICS KRISZTINA; FISCHER JANOS; LEVAI SANDOR; ERDELYI PETER
摘要:This invention relates to a process for the synthesis of mosapride citrate represented by the formula (I) and having the chemical name: (R, S) -4-amino-5-chloro-2-ethoxy-N - {- citrate dihydrate 4- (4-fluoro-benzyl) -2-morpholinyl] methyl} benzamide. The method of this invention comprises reacting the compound represented by formula (II) with di-tert-butyl-dicarbonate in an alcohol in the presence of a base; ethylating the product obtained in an inert solvent in the presence of a base; then hydrolyzing the compound obtained with an alkyl hydroxide and neutralizing the salt obtained with an acid. This process then consists in chlorinating the product obtained, then reacting the compound obtained represented by formula (VI) with the compound represented by formula (VII) in which BOC denotes a protective group of tert-butoxy-carbonyl; and removing the protecting group from the compound obtained represented by the formula (VIII) in which BOC is as defined above. It is then a question of preparing the mosapride base, and optionally of producing, by means of an acid and preferably citric acid, a pharmaceutically acceptable salt, preferably the mosapride citrate dihydrate represented by the formula (I ).

专利号:EP-1515958-A2
优先权日:2002-06-13
标 题:Process for the synthesis of mosapride

专利号:WO-03106440-A2
优先权日:2002-06-13
标题:Process for the synthesis of a benzamide derivative