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【结 构 式】

【药物名称】

【化学名称】4-[3-(4-Benzylpiperidin-1-yl)-1-propynyl]phenol

【CA登记号】

【 分 子 式 】C21H23NO

【 分 子 量 】305.42356

【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 propargyl tosylate (II) to afford the N-propynyl piperidine (III). Subsequent coupling of (III) with 4-iodophenol (IV) in the presence of Pd(PPh3)4 in pyrrolidine produced the corresponding propynyl 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.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 26225 4-benzylpiperidine 31252-42-3 C12H17N 详情 详情
(II) 26226 2-propynyl 4-methylbenzenesulfonate C10H10O3S 详情 详情
(III) 26227 4-benzyl-1-(2-propynyl)piperidine C15H19N 详情 详情
(IV) 22242 4-iodophenol 540-38-5 C6H5IO 详情 详情
Extended Information