ML-10375
苯甲酸,4-氨基-5-氯-2-甲氧基-, 2-[(3R,5S)-3,5-二甲基-1-哌啶基]乙基酯,rel-Chemical Name: cis-4-Amino-2-methoxy-5-chlorobenzoic acid 2-(3,5-dimethylpiperidin-1-yl)ethyl ester
CAS No. 174008-52-7, 174008-51-6 (trans-isomer), 174008-53-8 (undefined isomer), 174008-54-9 (undefined isomer, monoHCl salt)
项目整合开发状态: Biological Testing
项目研究机构: Sanofi-Aventis (Originator)
合成路线:Reaction of 4-amino-5-chloro-2-methoxybenzoic acid (I) with 1,2-dibromoethane in the presence of 1,8-diazabicyclo[5.4.0]undec-7-ene afforded bromoethyl ester (II).This was then condensed with a mixture of cis and trans 3,5-dimethylpiperidines (III),and the resulting mixture of amines was finally separated by column chromatogaphy to provide the target cis compound.
📌 参考资料/链接：
参考文献标题:Esters of 4-amino-5-chloro-2-methoxybenzoic acid,process for their preparation and pharmaceutical compsns.containing them
文献作者:Langlois,M.; Guzzi,U.; Cecchi,R.; Croci,T.(Midy SpA)
参考来源:EP 0683161
📄 详细内容
合成路线:Reaction of 4-amino-5-chloro-2-methoxybenzoic acid (I) with 1,2-dibromoethane in the presence of 1,8-diazabicyclo[5.4.0]undec-7-ene afforded bromoethyl ester (II).This was then condensed with a mixture of cis and trans 3,5-dimethylpiperidines (III),and the resulting mixture of amines was finally separated by column chromatogaphy to provide the target cis compound.
参考文献标题:New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors
文献作者:Yang,D.; Soulier,J.-L.; Sicsic,S.; Mathe-Allainmat,M.; Bremont,B.; Croci,T.; Cardamone,R.; Aureggi,G.; Langlois,M.
参考来源:J Med Chem 1997,40(4),608
产品链接: CAS No. 174008-52-7››