CAS: 112885-42-4; 4-Amino-5-Chloro-2-Ethoxy-N-((4-(4-Fluorobenzyl)Morpholin-2-yl)Methyl)Benzamide 2-Hydroxypropane-1,2,3-Tricarboxylate

上下游产品

CAS号112885-41-3 莫沙必利 | CAS号77-92-9 柠檬酸 | CAS号112885-41-3 莫沙必利

(Rs)-4-Amino-5-Chloro-2-Ethoxy-N-{[4-(4-Fluoro-Benzyl)-2-Morpholinyl]-Methyl}-Benzamide Trifluoroacetate置于sodium Hydroxide,柠檬酸体系中,用 二氯甲烷,水 用作溶剂,以83%的收率获得4-氨基-5-氯-2-乙氧基-N-[[4-(4-氟苄基)-2-吗啉基]甲基]苯甲酰胺枸橼酸盐
参考文献: Process For The Synthesis Of Mosapride[fr] Procede De Synthese D'Un Derive Benzamide
标题: Process For The Synthesis Of Mosapride[fr] Procede De Synthese D'Un Derive Benzamide

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:CN-101538217-A
优先权日:2008-03-20
标 题:A new method for the synthesis of 2-ethoxy-4-amino-5-chlorobenzoic acid and its intermediates

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

专利号:CN-108862767-A
优先权日:2018-07-04
标 题 :Wastewater treatment device and process of mosapride citrate impurity synthesis process

专利号:CN-101538217-B
优先权日:2008-03-20
标 题 :Novel synthesis method of 2-ethoxy-4-amino-5-chlorobenzoic acid and intermediate thereof