Raclopride, A-40664(tartrate)
雷氯必利Chemical Name: (S)-3,5-Dichloro-N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-hydroxy-6-methoxybenzamide
CAS No. 84225-95-6
项目整合开发状态: Phase II
项目研究机构: AstraZeneca (Originator)
合成路线:The reaction of 3-chloro-5-ethyl-2,6-dimethoxybenzoic acid (I) with SOCl2 gives the corresponding acyl chloride (II),which is condensed with N-ethyl-2-(aminomethyl)pyrrolidine (III) in refluxing CHCl3 yielding N-ethyl-2-(3-chloro-5-ethyl-2,6-dimethoxybenzamidomethyl)pyrrolidine (IV).Finally,this compound is treated with BBr3 in methylene chloride.
合成路线:The reaction of 3,5-dichloro-6-methoxysaliclic acid (I) with refluxing SOCl2 gives the corresponding acyl chloride (II),which is condensed with 1-ethyl-2-(aminomethyl)pyrrolidine (III) in methylene chloride yielding the amide (IV).Finally,this compound is partially demethylated with BBr3 in methylene chloride ether.
📌 参考资料/链接：
参考文献标题:Benzamido-derivatives
文献作者:Florvall,G.L.; Lundstroem,J.O.G.; Raemsby,S.I.; Oegren,S.O.(AstraZeneca plc)
参考来源:DD 201886; EP 0060235; JP 57159762; US 4789683
📄 详细内容
合成路线:The reaction of 3,5-dichloro-6-methoxysaliclic acid (I) with refluxing SOCl2 gives the corresponding acyl chloride (II),which is condensed with 1-ethyl-2-(aminomethyl)pyrrolidine (III) in methylene chloride yielding the amide (IV).Finally,this compound is partially demethylated with BBr3 in methylene chloride ether.
参考文献标题:Raclopride
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1986,11(5),387
合成路线:The reaction of 3,5-dichloro-6-methoxysaliclic acid (I) with refluxing SOCl2 gives the corresponding acyl chloride (II),which is condensed with 1-ethyl-2-(aminomethyl)pyrrolidine (III) in methylene chloride yielding the amide (IV).Finally,this compound is partially demethylated with BBr3 in methylene chloride ether.
参考文献标题:Potential neuroleptic agents.4.Chemistry,behavioral pharmacology,and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides
文献作者:de Paulis,T.; Kumar,Y.; Johansson,L.; Ramsby,S.; Hall,H.; Sallemark,M.; Angeby-Moller,K.; Ogren,S.O.
参考来源:J Med Chem 1986,29(1),61
产品链接: CAS No. 84225-95-6››