【药物名称】Raclopride, A-40664(tartrate)
化学结构式(Chemical Structure):
参考文献No.42024
标题:Benzamido-derivatives
作者:Florvall, G.L.; Lundstroem, J.O.G.; Raemsby, S.I.; Oegren, S.O. (AstraZeneca plc)
来源:DD 201886; EP 0060235; JP 57159762; US 4789683
合成路线图解说明:

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.

合成路线图解说明:

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No.49735
标题:Raclopride
作者:Prous, J.; Casta馿r, J.
来源:Drugs Fut 1986,11(5),387
合成路线图解说明:

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No.558622
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
作者:de Paulis, T.; Kumar, Y.; Johansson, L.; Ramsby, S.; Hall, H.; Sallemark, M.; Angeby-Moller, K.; Ogren, S.O.
来源:J Med Chem 1986,29(1),61
合成路线图解说明:

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.

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