Pinacidil, S-1230, P-1134, Pindac
吡那地尔 吡那地尔 Chemical Name: (?-N'-Cyano-N-4-pyridinyl-N''-(1,2,2-trimethylpropyl)guanidine monohydrate
CAS No. 85371-64-8, 60560-33-0 (anhydrous)
项目整合开发状态: Launched-1987
项目研究机构: Leo (Originator)
合成路线:This compound can be obtained in two related ways:1) By reaction of N-(4-pyridyl)-N'-(1,2,2-trimethylpropyl)thiourea (I) with cyanamide (II) by means of dicyclohexylcarbodiimide (DCC) and ethyldiisopropylamine in ether.2) The reaction of (I) with phosgene in toluene - THF by means of ethyldiisopropylamine in THF gives N-(4-pyridyl)-N'-(1,2,2-trimethylpropyl)carbodiimide (III),which is condensed with (II) by means of ethyldiisopropylamine.
合成路线:Thiourea (III) was prepared by condensation of 3-pyridyl isothiocyanate (I) with 1,1-dimethylpropyl amine (II).Desulfuration of thiourea (III) by means of phosgene and diisopropyl ethylamine,or triphenylphosphine and CCl4 gave rise to the carbodiimide (IV).Finally,addition of cyanamide to carbodiimide (IV) furnished the target N-cyanoguanidine derivative
📌 参考资料/链接：
参考文献标题:Antihypertensive pyridylguanidine compounds
文献作者:Petersen,H.J.(Leo Pharmaceutical Products Ltd.A/S)
参考来源:DE 2557438; FR 2294703; GB 1489879; JP 51086474; US 4057636
📄 详细内容
合成路线:This compound can be obtained in two related ways:1) By reaction of N-(4-pyridyl)-N'-(1,2,2-trimethylpropyl)thiourea (I) with cyanamide (II) by means of dicyclohexylcarbodiimide (DCC) and ethyldiisopropylamine in ether.2) The reaction of (I) with phosgene in toluene - THF by means of ethyldiisopropylamine in THF gives N-(4-pyridyl)-N'-(1,2,2-trimethylpropyl)carbodiimide (III),which is condensed with (II) by means of ethyldiisopropylamine.
参考文献标题:P-1134
文献作者:Blancafort,P.; Castar,J.; Serradell,M.N.; Hopkins,S.J.
参考来源:Drugs Fut 1981,6(3),149
产品链接: CAS No. 85371-64-8›› 产品链接: CAS No.60560-33-0››