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【结 构 式】

【分子编号】10003

【品名】2-([2-[(2-Furylmethyl)sulfanyl]ethyl]amino)-5-[(6-methyl-3-pyridinyl)methyl]-4(3H)-pyrimidinone

【CA登记号】72717-05-6

【 分 子 式 】C18H20N4O2S

【 分 子 量 】356.44856

【元素组成】C 60.65% H 5.66% N 15.72% O 8.98% S 9%

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)

A new synthesis of lupitidine has been described: The condensation of 5-(2-methylpyridin-5-yl)-2-(nitroamino)pyrimidin-4(3H)-one (I) with 2-(2-furylmethylthio)ethylamine (II) in refluxing pyridine gives 2-[2-(2-furylmethylthio)ethylamino]-5-(2-methylpyridin-5-ylmethyl)pyrimidin-4(3H)-one (III), which is then submitted to a conventional Mannich condensation with formaldehyde and dimethylamine in acetic acid.

1 Parsons, M.E.; Rawlings, D.A.; Ife, R.J.; Brown, T.H.; Blakemore, R.C.; Blurton, P.; Armitage, M.A.; Durant, G.J.; Slingsby, B.P.; Ganellin, C.R.; Isocytosine H2-receptor histamine antagonists. III. The synthesis and biological activity of lupitidine (SK&F 93479) and related compounds. Eur J Med Chem 1990, 25, 217-26.
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) 10001 5-(2-Methylpyridin-5-yl)-2-(nitroamino)pyrimidin-4(3H)-one 72716-93-9 C11H11N5O3 详情 详情
(II) 10002 2-[(2-Furylmethyl)sulfanyl]-1-ethanamine; 2-[(2-Furylmethyl)sulfanyl]ethylamine; 2-(2-Aminoethyl) furfuryl thiol ether 36415-21-1 C7H11NOS 详情 详情
(III) 10003 2-([2-[(2-Furylmethyl)sulfanyl]ethyl]amino)-5-[(6-methyl-3-pyridinyl)methyl]-4(3H)-pyrimidinone 72717-05-6 C18H20N4O2S 详情 详情
Extended Information