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【结 构 式】 
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【药物名称】FR-252384 【化学名称】9-Methyl-2-(3-pyridyl)-3,4,5,6-tetrahydrobenzo[3,4]cyclohepta[1,2-d]imidazole 【CA登记号】 【 分 子 式 】C18H17N3 【 分 子 量 】275.35629 |
【开发单位】Fujisawa (Originator) 【药理作用】Antiobesity Drugs, METABOLIC DRUGS, Treatment of Nutritional Disorders, Neuropeptide Y5 (NPY Y5) Antagonists |
合成路线1
Nitrosation of the benzocycloheptanone (I) with isoamyl nitrite furnishes the keto oxime (II). Subsequent ring closure of (II) with pyridine-3-carboxaldehyde (III) and ammonium acetate produces the N-hydroxy imidazole derivative (IV). Then, reduction of the N-hydroxy group of (IV) is performed by treatment PCl3 in DMF
| 【1】 Satoh, Y.; Hatori, C.; Ito, H.; Novel potent antagonists of human neuropeptide Y-Y5 receptor. Part 4: Tetrahydrodiazabenzazulene derivatives. Bioorg Med Chem Lett 2002, 12, 7, 1009. |
| 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) | 60801 | 3-methyl-5,7,8,9-tetrahydro-6H-benzo[a]cyclohepten-6-one | C12H14O | 详情 | 详情 | |
| (II) | 60802 | 3-methyl-8,9-dihydro-5H-benzo[a]cycloheptene-5,6(7H)-dione 5-oxime | C12H13NO2 | 详情 | 详情 | |
| (III) | 12849 | Nicotinaldehyde; 3-Pyridinecarboxaldehyde | 500-22-1 | C6H5NO | 详情 | 详情 |
| (IV) | 60803 | 9-methyl-2-(3-pyridinyl)-5,6-dihydrobenzo[3,4]cyclohepta[1,2-d]imidazol-1(4H)-ol | C18H17N3O | 详情 | 详情 |
Extended Information