ZK-811752, BX-471
ZK-811752(BX471)抑制剂 (2R)-1-[[[4-氯-2-(脲基)苯氧基]甲基]羰基]-2-甲基-4-(4-氟苄基)哌嗪 Chemical Name: N-[5-Chloro-2-[2-[4-(4-fluorobenzyl)-2(R)-methylpiperazin-1-yl]-2-oxoethoxy]phenyl]urea hydrochloride
CAS No. 288262-96-4, 217645-70-0 (free base)
项目整合开发状态: Phase II
项目研究机构: Berlex (Originator)
合成路线:Condensation of chloroacetyl derivative (I) with phenolic compound (II) by means of K2CO3 in DMF affords the desired compound.
合成路线:Alkylation of (R)-2-methylpiperazine (I) with 4-fluorobenzyl bromide (II) provides 1-(4-fluorobenzyl)-3-methylpiperazine (III).Subsequent acylation of piperazine (III) with (4-chlorophenoxy)acetyl chloride (IV) furnishes the title amide.
合成路线:In a further method,1-(4-fluorobenzyl)-3-methylpiperazine (I) is acylated by chloroacetyl chloride to provide the chloroacetamide (II).Subsequent chloride displacement with 4-chlorophenol (III) leads to the target chlorophenoxy acetamide.
📌 参考资料/链接:
参考文献标题:Piperazine derivs.and their use as anti-inflammatory agents
文献作者:Monahan,S.D.; Xu,W.; Morissey,M.M.; Bauman,J.G.; Ng,H.P.; Hesselgesser,J.E.; Liang,M.; Zheng,W.; Islam,I.; May,K.B.; Ghannam,A.F.; Buckman,B.O.; Horuk,R.; Wei,G.P.(Schering AG)
参考来源:US 6207665; WO 9856771