CHS-828
Chemical Name: N-[6-(4-Chlorophenoxy)hexyl]-N'-cyano-N''-(4-pyridyl)guanidine
项目整合开发状态: Phase II
项目研究机构: Leo (Originator)
合成路线:The condensation of pyridin-4-ylamine (I) with the iminodithiocarbonate (II) by means of NaH in DMF gives the isothiourea (III),which is finally condensed with 6-(4-chlorophenoxy)hexylamine (IV) by means of TEA in pyridine.Alternatively,the target guanidine can also be obtained by condensation of N-[6-(4-chlorophenoxy)hexyl]-N'-(4-pyridyl)thiourea (V) with cyanamide by means of DCC and TEA in acetonitrile.
📌 参考资料/链接：
参考文献标题:N-Cyano-N'-pyridylguanidines as serotonin antagonists
文献作者:Bramm,E.; Petersen,H.H.J.(Leo Pharmaceutical Products Ltd.A/S)
参考来源:EP 0660823; JP 1996501539; US 5563160; US 5696140; WO 9406770
📄 详细内容
合成路线:The condensation of pyridin-4-ylamine (I) with the iminodithiocarbonate (II) by means of NaH in DMF gives the isothiourea (III),which is finally condensed with 6-(4-chlorophenoxy)hexylamine (IV) by means of TEA in pyridine.Alternatively,the target guanidine can also be obtained by condensation of N-[6-(4-chlorophenoxy)hexyl]-N'-(4-pyridyl)thiourea (V) with cyanamide by means of DCC and TEA in acetonitrile.
参考文献标题:Novel cyanoguanidines with potent oral antitumor activity
文献作者:Schou,C.; et al.
参考来源:Bioorg Med Chem Lett 1997,7(24),3095