【药物名称】Lerisetron, F-0930-RS
化学结构式(Chemical Structure):
参考文献No.19272
标题:New 2-piperazinylbenzimidazole derivs.
作者:Orjales-Venero, A.; Garcia-Dominguez, N.; Rubio-Royo, V.; Rodes-Solanes, R. (FAES)
来源:EP 0512939; JP 1995002795; US 5256665
合成路线图解说明:

N-Alkylation of 2-chlorobenzimidazole (I) with benzyl bromide (II) by means of NaH in DMF provides benzylated derivative (III), which is converted into the desired compound by heating with piperazine (IV).

参考文献No.412390
标题:New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation
作者:Orjales, A.; Mosquera, R.; Labeaga, L.; Rodes, R.
来源:J Med Chem 1997,40(4),586
合成路线图解说明:

N-Alkylation of 2-chlorobenzimidazole (I) with benzyl bromide (II) by means of NaH in DMF provides benzylated derivative (III), which is converted into the desired compound by heating with piperazine (IV).

参考文献No.629156
标题:5-HT3R binding of lerisetron: An interdisciplinary approach to drug-receptor interactions
作者:Parihar, H.S.; Suryanarayanan, A.; Ma, C.; Joshi, P.; Venkataraman, P.; Schulte, M.K.; Kirschbaum, K.S.
来源:Bioorg Med Chem Lett 2001,11(16),2133
合成路线图解说明:

N-Alkylation of 2-chlorobenzimidazole (I) with benzyl bromide (II) by means of NaH in DMF provides benzylated derivative (III), which is converted into the desired compound by heating with piperazine (IV).

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