YM-176770
Chemical Name: 1-[6-[2-[3-(4-Biphenylyl)-5-methyl-4H-1,2,4-triazol-4-yl]phenoxy]hexyl]-4-methylpiperazine
CAS No. 258878-50-1
项目整合开发状态: Preclinical
项目研究机构: Yamanouchi (Originator)
合成路线:Acetylation of o-aminophenol (I) gives o-hydroxy acetanilide (II),which is then protected as the benzyl ether (III) with benzyl bromide and K2CO3.Treatment of acetamide (III) with P2S5 affords the corresponding thioamide (IV),and subsequent S-methylation of (IV) gives rise to the thioimidate (V).Cyclization of thioimidate (V) with 4-biphenylcarboxylic acid hydrazide (VI) in hot DMF leads to the triazole derivative (VII).After benzyl group hydrogenolysis in (VII),the resultant phenol (VIII) is alkylated with 1,6-dibromohexane (IX) to produce the bromohexyl ether (X).Finally,condensation of bromide (X) with N-methylpiperazine (XI) furnishes the title compound.
📌 参考资料/链接：
参考文献标题:Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V1A receptor
文献作者:Kakefuda,A.; Suzuki,T.; Tobe,T.; Tsukada,J.; Tahara,A.; Sakamoto,S.; Tsukamoto,S.
参考来源:J Med Chem 2002,45(12),2589