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【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.
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) 26228 3-butynyl 4-methylbenzenesulfonate 23418-85-1 C11H12O3S 详情 详情
(III) 26229 4-benzyl-1-(3-butynyl)piperidine C16H21N 详情 详情
(IV) 22242 4-iodophenol 540-38-5 C6H5IO 详情 详情
Extended Information