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【结 构 式】 
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【分子编号】40187 【品名】N-cyanoethyl-3-spiro(2-ethylenedioxy)oxindole 【CA登记号】 |
【 分 子 式 】C13H12N2O3 【 分 子 量 】244.24996 【元素组成】C 63.93% H 4.95% N 11.47% O 19.65% |
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 reduction of 2'-oxospiro-(1,3-dioxolane-2,3'-indoline)-1'-propionitrile (V) with H2 over Raney-Ni in NH3 saturated ethanol gives 2'-oxospiro-(1,3-dioxolane-2,3'-indoline)-1'-propanamine (VI), which, without isolation, is cyclized in refluxing xylene yielding 3',4'-dihydrospiro[1,3-dioxolane-2,10'(2H,10H)pyrimido-[1,2-a]indole] (VII). The hydrolysis of (VII) with aqueous HCl at 85 C affords 3,4-dihydropyrimido[1,2-a]indole-10(2H)-one (VIII), which is finally treated with m-chlorophenylmagnesium bromide (IX) in refluxing ethyl ether.
| 【1】 White, A.C.; Black, R.M. (John Wyeth & Brother Ltd.); Fused ring indole derivatives. DE 2200584; ES 398678; ES 409296; FR 2121699; GB 1366133 . |
| 【2】 Weetman, D.F.; Castaner, J.; Ciclazindol. Drugs Fut 1977, 2, 8, 508. |
Extended Information