Lerisetron, F-0930-RS
来立司琼Chemical Name: 1-Benzyl-2-(1-piperazinyl)benzimidazole
CAS No. 143257-98-1
项目整合开发状态: Phase III
项目研究机构: FAES (Originator), PharmaMar (Licensee)
合成路线: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).
📌 参考资料/链接：
参考文献标题:New 2-piperazinylbenzimidazole derivs.
文献作者:Orjales-Venero,A.; Garcia-Dominguez,N.; Rubio-Royo,V.; Rodes-Solanes,R.(FAES)
参考来源:EP 0512939; JP 1995002795; US 5256665
📄 详细内容
合成路线: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).
参考文献标题:New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists.Synthesis and pharmacological evaluation
文献作者:Orjales,A.; Mosquera,R.; Labeaga,L.; Rodes,R.
参考来源:J Med Chem 1997,40(4),586
合成路线: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).
参考文献标题:5-HT3R binding of lerisetron: An interdisciplinary approach to drug-receptor interactions
文献作者:Parihar,H.S.; Suryanarayanan,A.; Ma,C.; Joshi,P.; Venkataraman,P.; Schulte,M.K.; Kirschbaum,K.S.
参考来源:Bioorg Med Chem Lett 2001,11(16),2133
产品链接: CAS No. 143257-98-1››