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【结 构 式】

【分子编号】43368

【品名】2-(2-oxo-1-piperidinyl)acetic acid

【CA登记号】

【 分 子 式 】C7H11NO3

【 分 子 量 】157.16928

【元素组成】C 53.49% H 7.05% N 8.91% O 30.54%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(VII)

Alkylation of delta-valerolactam (V) with tert-butyl bromoacetate in the presence of NaH provided (VI). Subsequent tert-butyl ester cleavage by means of trifluoroacetic acid furnished 2-(2-oxopiperidin-1-yl)acetic acid (VII), which was finally coupled with amine (IV) to afford the title amide.

1 Murray, W.V.; Jolliffe, L.; Pulito, V.; Li, X.; Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists. Bioorg Med Chem Lett 2000, 10, 10, 1093.
2 Mulcahy, L.; Pulito, V.; Villani, F.; Li, X.; Murray, W.; Maryanoff, C.; Jolliffe, L.; Reitz, A. (Ortho-McNeil Pharmaceutical, Inc.); Arylsubstd. piperazines useful in the treatment of benign prostatic hyperplasia. EP 0984777; US 6071915; WO 9851298 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(IV) 43365 2-[4-(2-isopropoxyphenyl)-1-piperazinyl]ethylamine; 2-[4-(2-isopropoxyphenyl)-1-piperazinyl]-1-ethanamine C15H25N3O 详情 详情
(V) 43366 2-piperidinone 675-20-7 C5H9NO 详情 详情
(VI) 43367 tert-butyl 2-(2-oxo-1-piperidinyl)acetate C11H19NO3 详情 详情
(VII) 43368 2-(2-oxo-1-piperidinyl)acetic acid C7H11NO3 详情 详情
Extended Information