【结 构 式】 |
【分子编号】33684 【品名】N'-hydroxy-3-pyridinecarboximidamide 【CA登记号】 |
【 分 子 式 】C6H7N3O 【 分 子 量 】137.1412 【元素组成】C 52.55% H 5.14% N 30.64% O 11.67% |
与该中间体有关的原料药合成路线共 3 条
合成路线1
该中间体在本合成路线中的序号:(IV)N-(2,3-Epoxypropyl)piperidine (III), prepared from piperidine (I) and epichlorhydrin (II), was condensed with nicotinic acid amidoxime (IV) in the presence of basic catalysts, such as NaOH, t-BuOK, Al2O3 or SnO2, in hot DMF to provide the title compound, which was finally converted to the dihydrochloride salt.
【1】 Somfai, E,; Bertok, B.; Szekely, I.; Takacs, K.; Thurner, A.; Gajary, A.; Botar, S.; Nagy, L. (Chinoin Pharmaceutical and Chemical Works Co., Ltd.); Improved process for the preparation of amidoxime derivs.. WO 9008131 . |
合成路线2
该中间体在本合成路线中的序号:(IV)Alternatively, the title compound was prepared by condensation of nicotinamidoxime (IV) with 1,1-pentamethylene-3-hdroxyazetidinium chloride (V).
【1】 Somfai, E,; Bertok, B.; Szekely, I.; Takacs, K.; Thurner, A.; Gajary, A.; Botar, S.; Nagy, L. (Chinoin Pharmaceutical and Chemical Works Co., Ltd.); Improved process for the preparation of amidoxime derivs.. WO 9008131 . |
合成路线3
该中间体在本合成路线中的序号:(IV)In a further procedure, nicotinamidoxime (IV) was condensed with 1-chloro-3-piperidino-2-propanol (VI) in the presence of ethanolic NaOEt.
【1】 Farago, K.; Literati, P.N.; Simay, A.; Takacs, K.; Virag, S.; Szcntivanyi, M.; Kiss, I. (Chinoin Pharmaceutical and Chemical Works Co., Ltd.); O-(3-Amino-2-hydroxy-propyl)amidoxime derivs., process for the preparation thereof and pharmaceutical compsns. containing same. US 4308399 . |
Extended Information