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【结 构 式】

【药物名称】Centbucridine, CDRI-64/124

【化学名称】N-(Butylamino)-1,2,3,4-tetrahydroacridine hydrochloride

【CA登记号】34811-20-6, 316-15-4 (free base)

【 分 子 式 】C17H23ClN2

【 分 子 量 】290.83926

【开发单位】

【药理作用】 

合成路线1

Anthranitic acid (I) is reacted with cyclohexanone (II) to give 5-hydroxy-1,2,3,4-tetrahydroacridine (III). The hydroxy compound (III) is then reacted with phosphorous oxychloride to give 5-chloro-1,2,3,4-tetrahydroacridine (IV). Aminolysis of (IV) with n-butylamine affords centbucridine.

1 Arya, V.P.; Centbucridine. Drugs Fut 1980, 5, 6, 281.
2 Patnaik, G.K.; et al.; Studies in 4-substituted 2,3-polymethylene quinolines. CNS Drugs Ed. G.S. Sidhu, CSI, New Delhi .
3 Patnaik, G.K.; et al.; Compounds acting on the central nervous system. IV. 4-substituted 2,3-polymethylenequinolines. J Med Chem 1966, 9, 4, 483.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(A) 39041 butylamine; 1-butanamine 109-73-9 C4H11N 详情 详情
(I) 11661 2-Aminobenzoic acid;Anthranilic acid; o-Aminobenzoic acid 118-92-3 C7H7NO2 详情 详情
(II) 11059 Cyclohexanone 108-94-1 C6H10O 详情 详情
(III) 39040 1,2,3,4-tetrahydro-9-acridinol C13H13NO 详情 详情
(IV) 28181 9-chloro-1,2,3,4-tetrahydroacridine C13H12ClN 详情 详情
Extended Information