Y-39041
Chemical Name: N-[1-[4-[4-(2-Pyrimidinyl)-1-piperazinylmethyl]phenyl]cyclopropyl]acetamide
CAS No. 223511-88-4
项目整合开发状态: Preclinical
项目研究机构: Mitsubishi Pharma (Originator)
合成路线:Curtius rearrangement of 1-phenyl-1-cyclopropanecarboxylic acid (I) afforded amine (II),which was subsequently acetylated to produce amide (III) (1).Chloromethylation of (III) by means of chloromethyl methyl ether and TiCl4 gave rise to benzyl chloride (IV).This was finally condensed with pyrimidylpiperazine (V) in the presence of K2CO3 to yield the title compound.
📌 参考资料/链接：
参考文献标题:Piperazine cpds.and medicinal use thereof
文献作者:Adachi,K.; Moimoto,H.; Aoki,Y.; Hisadome,M.; Hanano,T.(Welfide Corporation)
参考来源:EP 1029851; WO 9919301
📄 详细内容
合成路线:Curtius rearrangement of 1-phenyl-1-cyclopropanecarboxylic acid (I) afforded amine (II),which was subsequently acetylated to produce amide (III) (1).Chloromethylation of (III) by means of chloromethyl methyl ether and TiCl4 gave rise to benzyl chloride (IV).This was finally condensed with pyrimidylpiperazine (V) in the presence of K2CO3 to yield the title compound.
参考文献标题:Novel DMARDs on the basis of a new concept of dual cytokine regulation,TNF-alpha suppression and IL-10 augmentation
文献作者:Hanano,T.; Adachi,K.; Aoki,Y.; Morimoto,H.; Naka,Y.; Hisadome,M.; Fukuda,T.; Sumichika,H.
参考来源:Bioorg Med Chem Lett 2000,10(9),881