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新产品编号:1088925

Chemical Name: 3-[4-(5-Methyl-4-phenylpyrazol-1-yl)piperidin-1-ylmethyl]benzonitrile
项目整合开发状态: Biological Testing
项目研究机构: Merck Sharp & Dohme (Originator)
合成路线:N-Boc-4-Hydroxypiperidine (I) was converted to the mesylate (II) with methanesulfonyl chloride and pyridine.Then,alkylation of 3-methyl-4-phenylpyrazole (III) with (II) in the presence of NaH yielded a mixture of regioisomeric pyrazoles (IV) and (V),which were separated using flash chromatography.The required isomer (IV) was subsequently treated with HCl in Et2O to remove the Boc protecting group.The resulting piperidine (VI) was finally alkylated with 3-(bromomethyl)benzonitrile (VII) to afford the title compound.
📌 参考资料/链接:
参考文献标题:4-N-Linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors
文献作者:Moore,K.W.; Bonner,K.; Jones,E.A.; Emms,F.; Leeson,P.D.; Marwood,R.; Patel,S.; Rowley,M.; Thomas,S.; Carling,R.W.
参考来源:Bioorg Med Chem Lett 1999,9(9),1285