Efletirizine, Ucb-28754-药物合成数据库

【药物名称】Efletirizine, Ucb-28754

化学结构式(Chemical Structure):

参考文献No.	3539
标题:	Novel 2-[4-(diphenylmethyl)-1-piperazinyl]acetic acids and their amides, process for their preparation and pharmaceutical compsns. Containing them
作者:	Baltes, E.; De Lannoy, J.; Rodriguez, L. (UCB SA)
来源:	EP 0058146; US 4525358

合成路线图解说明: The condensation of 1-(4-chlorodiphenylmethyl)piperazine (I) with methyl 2-(2-chloroethoxy)acetate (II) by means of Na2CO3 in refluxing xylene gives methyl 2-[2-[4-(4-chlorodiphenylmethyl)-1-piperazinyl]ethoxy]acetate (III), which is then hydrolyzed with KOH tn reftuxing ethanol.

合成路线图解说明: 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.

参考文献No.	410777
标题:	Efletirizine
作者:	Graul, A.; Leeson, P.; Casta馿r, R.M.
来源:	Drugs Fut 1997,22(6),626

合成路线图解说明: 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.