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【结 构 式】 
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【药物名称】OPC-14523 【化学名称】1-[3-[4-(3-Chlorophenyl)piperazin-1-yl]propyl]-5-methoxy-1,2,3,4-tetrahydroquinolin-2-one monomethanesulfonate 【CA登记号】145969-30-8 (free base), 145969-31-9 (monoHCl) 【 分 子 式 】C24H32ClN3O5S 【 分 子 量 】510.05674 |
【开发单位】Otsuka (Originator) 【药理作用】Antidepressants, Mood Disorders, Treatment of, PSYCHOPHARMACOLOGIC DRUGS, 5-HT1A Receptor Agonists |
合成路线1
The condensation of 5-methoxy-1,2,3,4-tetrahydroquinolin-2-one (I) with 1,3-dichloropropane (II) by means of NaH in DMF gives 1-(3-chloropropyl)-5-methoxy-1,2,3,4-tetrahydroquinolin-2-one (II), which is finally condensed with 1-(3-chlorophenyl)piperazine (IV) by means of NaI and K2CO3 in acetonitrile.
| 【1】 Oshiro, Y.; et al.; 3,4-Dihydro-2(1H)-quinolinone as a novel antidepressant drug: Synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4-dihydro-5-methoxy-2(1H)-quinolinone and its derivatives. J Med Chem 2000, 43, 2, 177. |
| 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) | 38679 | 5-methoxy-3,4-dihydro-2(1H)-quinolinone | C10H11NO2 | 详情 | 详情 | |
| (II) | 38680 | 1,3-dichloropropane | 142-28-9 | C3H6Cl2 | 详情 | 详情 |
| (III) | 38681 | 1-(3-chloropropyl)-5-methoxy-3,4-dihydro-2(1H)-quinolinone | C13H16ClNO2 | 详情 | 详情 | |
| (IV) | 22114 | 1-(3-chlorophenyl)piperazine | 6640-24-0 | C10H13ClN2 | 详情 | 详情 |
Extended Information