|
【结 构 式】 
|
【药物名称】 【化学名称】N'-(2-Chlorophenyl)-N-(3-ethynylphenyl)-2-oxopropanehydrazonamide 【CA登记号】 【 分 子 式 】C17H14ClN3O 【 分 子 量 】311.77363 |
【开发单位】Bristol-Myers Squibb (Originator) 【药理作用】Antidepressants, Anxiolytics, Mood Disorders, Treatment of, PSYCHOPHARMACOLOGIC DRUGS, CRF1 Antagonists |
合成路线1
2-Chloroaniline (I) is diazotized with NaNO2/HCl and the resultant diazonium salt (II) is further coupled to 2,4-pentanedione (III) to furnish the diketo hydrazone (IV). Subsequent bromination of (IV) with Br2 in Ac2O/AcOH gives rise to the hydrazonyl bromide (V). This is finally condensed with 3-ethynylaniline (VI) in DMF to provide the corresponding aryl amidrazone.
| 【1】 Wilson, D.M.; Termin, A.P.; Mao, L.; Ramirez-Weinhouse, M.M.; Molteni, V.; Gootenhuis, P.D.J.; Arylamidrazones as novel corticotropin releasing factor receptor antagonists. J Med Chem 2002, 45, 11, 2123. |
| 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) | 35804 | 2-chloroaniline; 2-chlorophenylamine | 95-51-2 | C6H6ClN | 详情 | 详情 |
| (II) | 63682 | 2-chlorobenzenediazonium chloride | C6H4Cl2N2 | 详情 | 详情 | |
| (III) | 11620 | 2,4-Pentanedione;acetylacetone | 123-54-6 | C5H8O2 | 详情 | 详情 |
| (IV) | 63683 | 2,3,4-pentanetrione 3-[N-(2-chlorophenyl)hydrazone] | C11H11ClN2O2 | 详情 | 详情 | |
| (V) | 63684 | N-(2-chlorophenyl)-2-oxopropanehydrazonoyl bromide | C9H8BrClN2O | 详情 | 详情 | |
| (VI) | 56445 | 3-Aminophenylacetylene; 3-Ethynylaniline; m-Aminophenylacetylene | 54060-30-9 | C8H7N | 详情 | 详情 |
Extended Information