ARM-434
Chemical Name: N,N-Diethyl-4-[1-(8-quinolyl)-1-(1-piperazinyl)methyl]benzamide
CAS No. 308110-21-6, 308110-65-8 (diHCl)
项目整合开发状态: Preclinical
项目研究机构: AstraZeneca (Originator)
合成路线:8-Bromoquinoline (I) is treated with sec-BuLi in THF to afford lithium derivative (II),which then reacts with carbaldehyde (III) in THF to provide alcohol (IV).Finally,(IV) is converted into the desired compound by chlorination with SOCl2 in CH2Cl2 followed by reaction with piperazine (V) in refluxing acetonitrile.
📌 参考资料/链接：
参考文献标题:New diarylmethylpiperazines as potent and selective nonpeptide delta opioid receptor agonists with increased in vitro metabolic stability
文献作者:Plobeck,N.; Delorme,D.; Wei,Z.-Y.; Yang,H.O.; Zhou,F.; Schwarz,P.; Gawell,L.; Gagnon,H.; Pelcman,B.; Schmidt,R.; Yue,S.Y.; Walpole,C.; Brown,W.; Zhou,E.; Labarre,M.; Payza,K.; St-Onge,S.; Kamassah,A.; Morin,P.E.; Projean,D.; et al.
参考来源:J Med Chem 2000,43(21),3878