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【结 构 式】 
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【药物名称】SPD-420, BDP-12, CX-516, Ampalex 【化学名称】6-(Piperidin-1-ylcarbonyl)quinoxaline 【CA登记号】154235-83-3 【 分 子 式 】C14H15N3O 【 分 子 量 】241.29515 |
【开发单位】University of California, Oakland (Originator), Cortex (Licensee), Organon (Licensee), Shire Pharmaceuticals (Licensee), Rush Presbyterian-St. Luke's Med. Center (Codevelopment), Servier (Codevelopment) 【药理作用】Alzheimer's Dementia, Treatment of , Antinarcoleptic Drugs, Antipsychotic Drugs, Attention Deficit Hyperactivity Disorder (ADHD), Treatment of, Autism, Treatment of, Cognition Disorders, Treatment of, NEUROLOGIC DRUGS, PSYCHOPHARMACOLOGIC DRUGS, Sleep Disorders, Treatment of, AMPA Receptor Modulators |
合成路线1
6-Quinoxalinecarboxylic acid (III) was prepared by condensation of 3,4-diaminobenzoic acid (I) with glyoxal (II). The title amide was then prepared by coupling of acid (III) with piperidine (VI) via formation of the mixed anhydride (IV) with pivaloyl chloride and Et3N or, alternatively, via activation of (III) as the imidazolide (V) by treatment with carbonyldiimidazole
| 【1】 Lynch, G.S.; Rogers, G.A. (University of California, Oakland); Drugs that enhance synaptic responses mediated by AMPA receptors. EP 1156043; JP 1995509468; WO 9402475 . |
| 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) | 62528 | C7H8N2O2 | 详情 | 详情 | ||
| (II) | 32557 | glyoxal; 2-oxoacetaldehyde | 107-22-2 | C2H2O2 | 详情 | 详情 |
| (III) | 62529 | 6-quinoxalinecarboxylic acid | C9H6N2O2 | 详情 | 详情 | |
| (IV) | 62530 | 1,1-dimethylpropanoic 6-quinoxalinecarboxylic anhydride | C14H14N2O3 | 详情 | 详情 | |
| (V) | 62531 | 1H-imidazol-1-yl(6-quinoxalinyl)methanone | C12H8N4O | 详情 | 详情 | |
| (VI) | 10158 | Piperidine | 110-89-4 | C5H11N | 详情 | 详情 |