Cetirizine hydrochloride, P-071, Alerlisin, Virlix, Reactine, Zyrtec

西替利嗪Chemical Name: (?-[2-[4-[(4-Chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid dihydrochloride
CAS No. 83881-51-0 (free base)
项目整合开发状态: Launched-1987
项目研究机构: UCB (Originator), Daiichi Pharmaceutical (Licensee), Lacer (Licensee), Menarini (Licensee), Pfizer (Licensee), Sanofi-Aventis (Licensee), Sumitomo Pharmaceuticals (Licensee)
合成路线: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: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.