【结 构 式】 |
【药物名称】 【化学名称】4-[4-(4-Benzylpiperidin-1-yl)-1-butynyl]phenol 【CA登记号】 【 分 子 式 】C22H25NO 【 分 子 量 】319.45065 |
【开发单位】Pfizer (Originator) 【药理作用】Antiparkinsonian Drugs, Extrapyramidal Disorders, Treatment of, NEUROLOGIC DRUGS, NMDA Antagonists |
合成路线1
4-Benzylpiperidine (I) was alkylated with butynyl tosylate (II) to afford the N-butynyl piperidine (III). Subsequent coupling of (III) with 4-iodophenol (IV) in the presence of Pd(PPh3)4 in pyrrolidine produced the corresponding butynyl phenol.
【1】 Bigge, C.F.; Serpa, K.; Wise, L.D.; Gregory, T.F.; Meltzer, L.T.; Wright, J.L.; Boxer, P.A.; Subtype-selective N-methyl-D-aspartate receptor antagonists: Synthesis and biological evaluation of 1-(arylakynyl)-4-benzylpiperidines. J Med Chem 1999, 42, 13, 2469. |
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