Tegaserod maleate, HTF-919, SDZ-HTF-919, Zelnorm, Zelmac
马来酸替加色罗 马来酸替加色罗 Chemical Name: 2-(5-Methoxy-1H-indol-3-ylmethylene)-N-pentylhydrazinecarboximidamide monomaleate; 1-(5-Methoxy-1H-indol-3-ylmethyleneamino)-3-pentylguanidine monomaleate
CAS No. 189188-57-6, 145158-71-0 (free base)
项目整合开发状态: Launched-2001
项目研究机构: Novartis (Originator), Bristol-Myers Squibb (Codevelopment)
合成路线:The alkylation of thiosemicarbazide (I) with methyl iodide in hot ethanol gives the corresponding S-methyl derivative (II),which is treated with pentylamine (III) in refluxing methanol to yield N1-amino-N3-pentylguanidine hydroiodide (IV).Finally,this compound is condensed with 5-methoxy-1H-indole-3-carbaldehyde (V) by means of HCl in methanol.
📌 参考资料/链接：
参考文献标题:Aminoguanidines
文献作者:Giger,R.K.A.; Mattes,H.(Novartis AG; Novartis Deutschland GmbH)
参考来源:EP 0505322; US 5510353
📄 详细内容
合成路线:The alkylation of thiosemicarbazide (I) with methyl iodide in hot ethanol gives the corresponding S-methyl derivative (II),which is treated with pentylamine (III) in refluxing methanol to yield N1-amino-N3-pentylguanidine hydroiodide (IV).Finally,this compound is condensed with 5-methoxy-1H-indole-3-carbaldehyde (V) by means of HCl in methanol.
参考文献标题:The serotonin 5-HT4 receptor.2.Structure-activity studies of the indole carbazimidamide class of agonists
文献作者:Buchheit,K.-H.; Gamse,R.; Giger,R.; Hoyer,D.; Klein,F.; Kl鰌pner,E.; Pfannkuche,H.-J.; Mattes,H.
参考来源:J Med Chem 1995,38(13),2331
合成路线:The alkylation of thiosemicarbazide (I) with methyl iodide in hot ethanol gives the corresponding S-methyl derivative (II),which is treated with pentylamine (III) in refluxing methanol to yield N1-amino-N3-pentylguanidine hydroiodide (IV).Finally,this compound is condensed with 5-methoxy-1H-indole-3-carbaldehyde (V) by means of HCl in methanol.
参考文献标题:Tegaserod Maleate
文献作者:Silvestre,J.S.; Graul,A.; Castar,J.
参考来源:Drugs Fut 1999,24(1),38
产品链接: CAS No. 189188-57-6›› 产品链接: CAS No.145158-71-0››