新产品编号:636473
Chemical Name: 2-(4-tert-Butyl-2,6-dimethylbenzyl)-1,4,5,6-tetrahydropyrimidine
CAS No. 246544-20-7, 246544-18-3 (hydrochloride)
项目整合开发状态: Biological Testing
项目研究机构: NPS Allelix (Originator), Virginia Commonwealth University (Originator)
合成路线:Alkylation of sodium cyanide with 4-tert-butyl-2,6-dimethylbenzyl chloride (I) afforded nitrile (II).Imidate (III) was then prepared by Pinner reaction of nitrile (II) with ethanolic HCl.Cyclization of (III) with 1,3-diaminopropane (IV) in ethanol furnished the desired cyclic amidine.In an alternative procedure,the target amidine was directly obtained by melting at 200 C nitrile (II) with the mono-tosylate salt of 1,3-diaminopropane.
📌 参考资料/链接：
参考文献标题:Imidazoles with serotonin receptor binding activity
文献作者:Glennon,R.A.; Law,H.(NPS Allelix Corp.; Virginia Commonwealth University)
参考来源:US 5969137; WO 9812183
📄 详细内容
合成路线:Alkylation of sodium cyanide with 4-tert-butyl-2,6-dimethylbenzyl chloride (I) afforded nitrile (II).Imidate (III) was then prepared by Pinner reaction of nitrile (II) with ethanolic HCl.Cyclization of (III) with 1,3-diaminopropane (IV) in ethanol furnished the desired cyclic amidine.In an alternative procedure,the target amidine was directly obtained by melting at 200 C nitrile (II) with the mono-tosylate salt of 1,3-diaminopropane.
参考文献标题:Imidazoline-modified benzylimidazolines as h5-HT1D/1B serotonergic ligands
文献作者:Prisinzano,T.; Law,H.; Dukat,M.; Slassi,A.; MacLean,N.; Demchyshyn,L.; Glennon,R.A.
参考来源:Bioorg Med Chem 2001,9(3),613