新产品编号:1981173
Chemical Name: 4-(Cyano-NNO-azoxy)-N-[6-[N2-cyano-N3-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]guanidino]hexyl]benzamide
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi "La Sapienza" (Originator), Universit?degli Studi di Milano (Originator), Universit?degli Studi di Torino (Originator), Universit?degli Studi Piemonte Orient. (Originator)
合成路线:Condensation of amine (I) with diphenyl cyanocarbonimidate (II) affords isourea (III),which is then converted into cyanoguanidine (V) by coupling with diamine (IV) in CH2Cl2.The final step for the synthesis of the desired product is the reaction of the primary amine group of (V) with the active ester (VI) obtained by activation of calvatic acid (VII) with N-hydroxysuccinimide (N-HOSu) and N,N'-dicyclohexyl-carbodiimide (DCC) in THF.
📌 参考资料/链接:
参考文献标题:Anti-Helicobacter pylori agents endowed with H2-antagonist properties
文献作者:Sorba,G.; Bertinaria,M.; Di Stilo,A.; Gasco,A.; Scaltrito,M.M.; Brenciaglia,M.I.; Dubini,F.
参考来源:Bioorg Med Chem Lett 2001,11(3),403
📄 详细内容
合成路线:Condensation of amine (I) with diphenyl cyanocarbonimidate (II) affords isourea (III),which is then converted into cyanoguanidine (V) by coupling with diamine (IV) in CH2Cl2.The final step for the synthesis of the desired product is the reaction of the primary amine group of (V) with the active ester (VI) obtained by activation of calvatic acid (VII) with N-hydroxysuccinimide (N-HOSu) and N,N'-dicyclohexyl-carbodiimide (DCC) in THF.
参考文献标题:Iodoaminopotentidine and related compounds: A new class of ligands with high affinity and selectivity for the histamine H2 receptor
文献作者:Hirschfeld,J.; Buschauer,A.; Elz,S.; Schunack,W.; Ruat,M.; Traiffort,E.; Schwartz,J.C.
参考来源:J Med Chem 1992,35(12),2231