【结 构 式】 |
【分子编号】60306 【品名】8-bromo-2-methyl-4-quinolinol 【CA登记号】 |
【 分 子 式 】C10H8BrNO 【 分 子 量 】238.08366 【元素组成】C 50.45% H 3.39% Br 33.56% N 5.88% O 6.72% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号:(I)In a related synthetic strategy, 8-bromo-4-hydroxy-2-methylquinoline (I) is converted to aryl triflate (II) by using N-phenyl trifluoromethanesulfonimide and NaH. Displacement of the triflate group of (II) with 1,2,3,6-tetrahydropyridine-4-carboxamide (III) gives the tetrahydropyridyl quinoline (IV). The bromoquinoline (IV) is finally subjected to Suzuki coupling with 2,4-dichlorophenylboronic acid (V) to produce the title compound
【1】 Kameo, K.; Kumagai, T.; Nakazato, A.; Okubo, T. (Taisho Pharmaceutical Co., Ltd.); Tetrahydropyridino or piperidino heterocyclic derivs.. EP 1299378; WO 0202549 . |
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) | 60306 | 8-bromo-2-methyl-4-quinolinol | C10H8BrNO | 详情 | 详情 | |
(II) | 60307 | 8-bromo-2-methyl-4-quinolinyl trifluoromethanesulfonate | C11H7BrF3NO3S | 详情 | 详情 | |
(III) | 60299 | 1,2,3,6-tetrahydro-4-pyridinecarboxamide | C6H10N2O | 详情 | 详情 | |
(IV) | 60308 | 1-(8-bromo-2-methyl-4-quinolinyl)-1,2,3,6-tetrahydro-4-pyridinecarboxamide | C16H16BrN3O | 详情 | 详情 | |
(V) | 48912 | 2,4-Dichlorophenylboronic acid; 2,4-Dichlorobenzeneboronic acid | 68716-47-2 | C6H5BCl2O2 | 详情 | 详情 |
Extended Information