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【结 构 式】 
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【药物名称】Ethyl loflazepate, CM-6912, Meilax, Victan 【化学名称】7-Chloro-3-ethoxycarbonyl-5-(2-fluorophenyl)-2-oxo-2,3-dihydro-1H-1,4-benzodiazepine 【CA登记号】29177-84-2 【 分 子 式 】C18H14ClFN2O3 【 分 子 量 】360.77528 |
【开发单位】Meiji Seika (Originator), Sanofi-synthélabo (Originator) 【药理作用】Anxiolytics, Generalized Anxiety Disorder (GAD), Treatment of, PSYCHOPHARMACOLOGIC DRUGS, Benzodiazepines |
合成路线1
2-Amino-5-chloro-2'-fluorobenzophenone (I) is condensed with monoethyl methoxycarbonyl aminomalonate (II) and the crude product obtained (III) is deprotected by HBr to give the free amine hydrobromide (IV). This product is then cyclized in a mixture of acetic acid-sodium acetate to obtain CM-6912, which is separated by filtration and recrystallized in ethanol.
| 【1】 Demarne, H.; Hallot, A.; Benzodiazepine derivatives and pharmaceutical compositions thereof. DE 2719608; FR 2350346; GB 1538164; JP 57081472; NL 7704911; NL 7704912; US 4235897 . |
| 【2】 Dubois, M.; Ethyl Loflazepate. Drugs Fut 1981, 6, 12, 772. |
| 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) | 32281 | 2-Amino-5-chloro-2'-fluorobenzophenone; (2-Amino-5-chlorophenyl)(2-fluorophenyl)methanone | 784-38-3 | C13H9ClFNO | 详情 | 详情 |
| (II) | 32282 | 3-ethoxy-N-(methoxycarbonyl)-3-oxoalanine | C7H11NO6 | 详情 | 详情 | |
| (III) | 32283 | ethyl 3-[4-chloro-2-(2-fluorobenzoyl)anilino]-2-[(methoxycarbonyl)amino]-3-oxopropanoate | C20H18ClFN2O6 | 详情 | 详情 | |
| (IV) | 32284 | ethyl 2-amino-3-[4-chloro-2-(2-fluorobenzoyl)anilino]-3-oxopropanoate | C18H16ClFN2O4 | 详情 | 详情 |