|
【结 构 式】 
|
【药物名称】YJA-20379-5 【化学名称】4,5-Dihydropyrido[1,2-a][1,3]thiazolo[5,4-g]benzimidazol-2-amine 【CA登记号】187680-75-7 【 分 子 式 】C12H10N4S 【 分 子 量 】242.3043 |
【开发单位】Yung-Jin (Originator) 【药理作用】Antiulcer Drugs, Gastric Antisecretory Drugs, GASTROINTESTINAL DRUGS, H+/K+-ATPase Inhibitors |
合成路线1
1,3-Cyclohexanedione (I) was brominated in cold water, and the resulting 2-bromo-1,3-cyclohexanedione (II) was condensed with 2-aminopyridine (III) in boiling EtOH to afford the dihydropyridobenzimidazolone (IV). Further bromination in concentrated HBr at 70 C gave bromoketone (V), which was finally condensed with thiourea (VI) in EtOH to yield the target tetracyclic compound.
| 【1】 Yoo, H.Y.; Chung, K.J.; Chai, J.P.; Chang, M.S.; Kim, S.G.; Choi, W.S.; Kim, Y.H.; Chun, J.K.; Chung, Y.K.; Kim, Y.H.; Paek, J.H.; Seo, K.H.; Kang, D.P. (Yung-Jin Pharmaceutical Co., Ltd.); Heterocycle-fused thiazole derivs.. EP 0843681; JP 1998508877; WO 9703076 . |
| 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) | 11244 | 1,3-Cyclohexanedione | 504-02-9 | C6H8O2 | 详情 | 详情 |
| (II) | 21027 | 2-bromo-1,3-cyclohexanedione | C6H7BrO2 | 详情 | 详情 | |
| (III) | 11305 | 2-Pyridinamine; 2-Pyridinylamine; 2-Aminopyridine | 504-29-0 | C5H6N2 | 详情 | 详情 |
| (IV) | 10180 | Thiourea | 62-56-6 | CH4N2S | 详情 | 详情 |
| (IV) | 21029 | 7,8-dihydropyrido[1,2-a]benzimidazol-9(6H)-one | C11H10N2O | 详情 | 详情 | |
| (V) | 21030 | 8-bromo-7,8-dihydropyrido[1,2-a]benzimidazol-9(6H)-one | C11H9BrN2O | 详情 | 详情 |
Extended Information