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【结 构 式】

【分子编号】34335

【品名】[8-(2-oxiranylmethoxy)-3,4-dihydro-1(2H)-quinolinyl](3-pyridinyl)methanone

【CA登记号】

【 分 子 式 】C18H18N2O3

【 分 子 量 】310.3526

【元素组成】C 69.66% H 5.85% N 9.03% O 15.47%

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:(V)

The acylation of 8-hydroxy-1,2,3,4-tetrahydroquinoline (I) with nicotinoyl chloride (II) by means of triethylamine in benzene gives 8-hydroxy-1-nicotinoyl-1,2,3,4-tetrahydroquinoline (III), which is condensed with epichlorohydrin (IV) by means of potassium tert-butoxide in DMF to yield 1-nicotinoyl-8-(2,3-epoxy-1-propoxy)-1,2,3,4-tetrahydroquinoline (V). Finally, this compound is condensed with isopropylamine (VI) in ethanol.

1 Graewinger, O.; Raabe, T.; Beyerle, R.; Scholtholt, J.; Nitz, R.E.; 1-Acyl-8-(3-amino-2-hydroxypropoxy)-1,2,3,4-tetrahydroquinolines, compositions and use. DD 153368; DE 2934609; EP 0025864; JP 56034668; US 4335123 .
2 Castaner, J.; Serradell, M.N.; Hillier, K.; Nicainoprol. Drugs Fut 1984, 9, 10, 749.
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) 16022 1,2,3,4-tetrahydro-8-quinolinol C9H11NO 详情 详情
(II) 10753 Nicotinoyl chloride C6H4ClNO 详情 详情
(III) 34334 [8-hydroxy-3,4-dihydro-1(2H)-quinolinyl](3-pyridinyl)methanone C15H14N2O2 详情 详情
(IV) 10146 Epichlorohydrin; 2-(Chloromethyl)oxirane 106-89-8 C3H5ClO 详情 详情
(V) 34335 [8-(2-oxiranylmethoxy)-3,4-dihydro-1(2H)-quinolinyl](3-pyridinyl)methanone C18H18N2O3 详情 详情
(VI) 23933 2-Propanamine; Isopropylamine 75-31-0 C3H9N 详情 详情
Extended Information