【结 构 式】 |
【分子编号】16023 【品名】(4-benzyl-1,4-oxazinan-2-yl)methyl 1,2,3,4-tetrahydro-8-quinolinyl ether; 8-[(4-benzyl-1,4-oxazinan-2-yl)methoxy]-1,2,3,4-tetrahydroquinoline 【CA登记号】 |
【 分 子 式 】C21H26N2O2 【 分 子 量 】338.44972 【元素组成】C 74.53% H 7.74% N 8.28% O 9.45% |
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:(III)The condensation of 4-benzyl-2-(chloromethyl)morpholine (I) with 8-hydroxy-1,2,3,4-tetrahydroquinoline (II) by means of NaH in hot DMF gives 8-(4-benzylmorpholin-2-ylmethoxy)-1,2,3,4-tetrahydroquinoline (III), which is methylated with methyl iodide and K2CO3 in refluxing acetone yielding the corresponding N-methyl derivative (IV). Finally, this compound is debenzylated by hydrogenolysis with H2 over Pd/C in ethanol.
【1】 Tracy, M.; Ngo, J.; Castaner, J.; Dabelotine Mesylate. Drugs Fut 1996, 21, 9, 890. |
【2】 Regnier, G.; Guillonneau, C.; Lepagnol, J. (ADIR et Cie.); Novel morpholine derivs., process for their preparation and pharmaceutical compsns. containing them. AU 8813520; EP 0286495; FR 2612926; JP 1988255279; US 4782054 . |
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) | 13396 | 4-Benzyl-2-(chloromethyl)morpholine | C12H16ClNO | 详情 | 详情 | |
(II) | 16022 | 1,2,3,4-tetrahydro-8-quinolinol | C9H11NO | 详情 | 详情 | |
(III) | 16023 | (4-benzyl-1,4-oxazinan-2-yl)methyl 1,2,3,4-tetrahydro-8-quinolinyl ether; 8-[(4-benzyl-1,4-oxazinan-2-yl)methoxy]-1,2,3,4-tetrahydroquinoline | C21H26N2O2 | 详情 | 详情 | |
(IV) | 16024 | 8-[(4-benzyl-1,4-oxazinan-2-yl)methoxy]-1-methyl-1,2,3,4-tetrahydroquinoline; (4-benzyl-1,4-oxazinan-2-yl)methyl 1-methyl-1,2,3,4-tetrahydro-8-quinolinyl ether | C22H28N2O2 | 详情 | 详情 |
Extended Information