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【结 构 式】

【分子编号】16842

【品名】methyl 2-(2-[4-[bis(4-fluorophenyl)methyl]piperazino]ethoxy)acetate

【CA登记号】

【 分 子 式 】C22H26F2N2O3

【 分 子 量 】404.4569264

【元素组成】C 65.33% H 6.48% F 9.39% N 6.93% O 11.87%

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)

Efletirizine can be obtained by two similar ways: 1) The condensation of 1-[bis(4-fluorophenyl)methyl]piperazine (I) with 2-(2-chloroethoxy)acetamide (II) by means of Na2CO3 in hot xylene gives 2-[2-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]ethoxy]acetamide (III), which is then hydrolyzed with 4N NaOH in refluxing ethanol. 2) The condensation of 1-[bis(4-fluorophenyl)methyl]piperazine (I) with 2-(2-chloroethoxy)acetic acid methyl ester (IV) by means of Na2CO3 in hot xylene gives 2-[2-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]ethoxy]acetic acid methyl ester amide (V), which is then hydrolyzed with 1N KOH in refluxing ethanol.

1 Graul, A.; Leeson, P.; Castañer, R.M.; Efletirizine. Drugs Fut 1997, 22, 6, 626.
2 Baltes, E.; De Lannoy, J.; Rodriguez, L. (UCB SA); Novel 2-[4-(diphenylmethyl)-1-piperazinyl]acetic acids and their amides, process for their preparation and pharmaceutical compsns. Containing them. EP 0058146; US 4525358 .
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) 16838 1-Bis(4-fluorophenyl)methyl piperazine; 1-[bis(4-fluorophenyl)methyl]piperazine 27469-60-9 C17H18F2N2 详情 详情
(II) 16839 2-(2-chloroethoxy)acetamide C4H8ClNO2 详情 详情
(III) 16840 2-(2-[4-[bis(4-fluorophenyl)methyl]piperazino]ethoxy)acetamide C21H25F2N3O2 详情 详情
(IV) 16841 methyl 2-(2-chloroethoxy)acetate C5H9ClO3 详情 详情
(V) 16842 methyl 2-(2-[4-[bis(4-fluorophenyl)methyl]piperazino]ethoxy)acetate C22H26F2N2O3 详情 详情
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