【结 构 式】 |
【分子编号】43367 【品名】tert-butyl 2-(2-oxo-1-piperidinyl)acetate 【CA登记号】 |
【 分 子 式 】C11H19NO3 【 分 子 量 】213.2768 【元素组成】C 61.95% H 8.98% N 6.57% O 22.51% |
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:(VI)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