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:US-4772618-A 优先权日:1985-08-06 标题:Benzamides 发明人:VEGA-NOVEROLA ARMANDO; PRIETO-SOTO JOSE M; PUJOL-NOGUERA FERNANDO; MORAGUES-MAURI JACINTO; SPICKETT ROBERT G W 权利人:FORDONAL SA 摘要:Substituted benzamides of the general formula I I in which: R represents an alkoxy, alkenyloxy or alkynyloxy group containing up to 7 carbon atoms in the group, R1 is hydrogen or a NR4R5, or NR6COR7 group, where R4, R5 and R6, which may be the same or different, is each hydrogen or an alkyl group and R7 is an alkyl or trifluoromethyl group, R2 is hydrogen, halogen, or a nitro, or sulphamoyl group, R3 represents hydrogen or a methyl or methoxy group, X represents a hydrocarbon chain containing 1 to 4 carbon atoms, one of which may optionally be replaced by an oxygen atom, Y represents a non-aromatic cyclic ether or a non-aromatic cyclic thioether group and pharmaceutically acceptable salts thereof are useful in the treatment of gastro-intestinal disorders. Various methods of synthesis are described including synthesis via novel amines of the formula IIIa which are themselves obtained by reduction of the corresponding oximes.
专利号:WO-2017185261-A1 优先权日:2016-04-27 标 题:Mosapride active metabolites, preparation method therefor, and applications thereof 发明人:ZHAO LONGSHAN; WANG SHAOJIE; HE ZHONGGUI; SONG YUFENG 权利人:UNIV SHENYANG PHARMACEUTICAL 摘要:The present invention relates to the technical field of medicine, and provides mosapride active metabolites (R)-N-[2-hydroxy-3-(4-fluorobenzyl)amino]propyl-5-chloro-4-amino-2-ethoxy benzamide (levo isomer) and (S)-N-[2-hydroxy-3-(4-fluorobenzyl)amino]propyl-5-chloro-4-amino-2-ethoxy benzamide (dextro isomer), salts thereof, a synthesis method for (R,S)-N-[2-hydroxy-3-(4-fluorobenzyl)amino]propyl-5-chloro-4-amino-2-ethoxy benzamide (racemate), and applications in gastrointestinal tract motility drug preparation. The present invention also relates to a drug composition comprising the three active ingredients and applications in gastrointestinal tract motility drug preparation. By means of the present invention, a mouse small intestine charcoal powder propelling model is used for respectively investigating the gastrointestinal motility promoting effects of the levo isomer, the dextro isomer and the racemate, and the results show that under the same dose, the activity of the levo isomer is relatively weak, the racemate and the dextro isomer have significant gastrointestinal motility promoting effects, and the activity of the dextro isomer is significantly surprior to the activity of the racemate.
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