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【结 构 式】

【药物名称】RX-72601

【化学名称】cis-1-[2-(3-Hydroxyphenyl)cyclohexyl]-1-methylpyrrolidinium bromide

【CA登记号】51572-98-6

【 分 子 式 】C17H26BrNO

【 分 子 量 】340.30687

【开发单位】

【药理作用】 

合成路线1

A mixture of 2-(3-methoxyphenyl)cyclohexanone (I), pyrrolidine (II) and formic acid is heated at 130-40 C to give cis-2-(3-methoxyphenyl)-1-pyrrolidylcyclohexane (III), which is demethylated with refluxing HBr (47%) giving cis-2-(3-hydroxyphenyl)-1-pyrrolidylcyclohexane (IV). Finally this tertiary amine is quaternized with CH3Br.

1 Castaner, J.; Hopkins, S.J.; RX 72601. Drugs Fut 1976, 1, 6, 304.
2 Singh, S.K.; Saibaba, V.; Ravikumar, V.; Rudrawar, S.V.; Daga, P.; Rao, C.S.; Akhila, V.; Hedge, P.; Rao, Y.K.; Synthesis and biological evaluation of 2,3-diarylpyrazines and quinoxalines as selective COX-2 inhibitors. J Pharm Pharmac 1974, 26, 8, 134.
3 Lewis, J.W. (Reckitt & Colman Pharmaceuticals); FR 2187296 .
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) 61376 2-(3-Methoxyphenyl)cyclohexanone 15547-89-4 C13H16O2 详情 详情
(II) 11376 Pyrrolidine 123-75-1 C4H9N 详情 详情
(III) 61377 1-[(1R,2R)-2-(3-methoxyphenyl)cyclohexyl]pyrrolidine; methyl 3-[(1R,2R)-2-(1-pyrrolidinyl)cyclohexyl]phenyl ether C17H25NO 详情 详情
(IV) 61378 3-[(1R,2R)-2-(1-pyrrolidinyl)cyclohexyl]phenol C16H23NO 详情 详情
Extended Information