【结 构 式】 |
【药物名称】SRA-880, NVP-SRA-880 【化学名称】1-[(3R,4aR,10aR)-6-Methoxy-1-methyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinolin-3-yl)-1-[4-(4-nitrophenyl)piperazin-1-yl]methanone malonate 【CA登记号】 【 分 子 式 】C29H36N4O8 【 分 子 量 】568.63227 |
【开发单位】Novartis (Originator) 【药理作用】Antipsychotic Drugs, Cognition Disorders, Treatment of, NEUROLOGIC DRUGS, PSYCHOPHARMACOLOGIC DRUGS, Somatostatin SRIF2A (sst1) Antagonists |
合成路线1
The benzoquinoline carboxylate ester (I) is hydrolyzed with NaOH to produce the sodium carboxylate salt (II). Activation of (II) with propane-phosphonic anhydride, followed by coupling with N-(4-nitrophenyl)piperazine (III) furnishes the corresponding amide.
【1】 Neumann, P.; Pfaeffli, P.; Seiler, M.P.; Swoboda, R. (Novartis AG; Novartis Deutschland GmbH); Benzo[g]quinoline derivs.. EP 0839136; JP 1999509197; US 5885988; WO 9703054 . |
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) | 61421 | methyl (4aS,10aR)-6-methoxy-1-methyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline-3-carboxylate | C17H23NO3 | 详情 | 详情 | |
(II) | 61422 | (4aS,10aR)-6-methoxy-1-methyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline-3-carboxylate | C16H20NO3 | 详情 | 详情 | |
(III) | 20299 | 1-(4-nitrophenyl)piperazine | 6269-89-2 | C10H13N3O2 | 详情 | 详情 |
Extended Information