BN-82451
4-[2-(氨基甲基)噻唑-4-盐]-2,6-二丁基苯醇二盐酸盐Chemical Name: 4-[2-(Aminomethyl)thiazol-4-yl]-2,6-di-tert-butylphenol dihydrochloride
CAS No. 335242-75-6
项目整合开发状态: Phase I
项目研究机构: Ipsen (Originator)
合成路线:Treatment of N-(carbobenzoxy)glycinamide (I) with Lawesson's reagent in boiling dioxane gives rise to the corresponding thioamide (II).This is then condensed with the bromoacetophenone (III) to produce thiazole (IV).Finally,alkaline hydrolysis of the carbamate group of (IV) furnishes the target primary amine.
📌 参考资料/链接：
参考文献标题:5-Membered heterocycle derivs.,production thereof and use thereof as medicaments
文献作者:Bigg,D.; Pommier,J.; Chabrier de Lassauniere,P.-E.; Thurieau,C.; Harnett,J.; Liberatore,A.-M.; Lannoy,J.(SCRAS (Societ?de Conseils de Recherches et d'Applications Scientifiques))
参考来源:EP 1223933; EP 1228760; JP 2003511416; WO 0126656
📄 详细内容
合成路线:Treatment of N-(carbobenzoxy)glycinamide (I) with Lawesson's reagent in boiling dioxane gives rise to the corresponding thioamide (II).This is then condensed with the bromoacetophenone (III) to produce thiazole (IV).Finally,alkaline hydrolysis of the carbamate group of (IV) furnishes the target primary amine.
参考文献标题:Phenolic thiazoles as novel orally-active neuroprotective agents
文献作者:Harnett,J.J.; Roubert,V.; Dolo,C.; Charnet,C.; Spinnewyn,B.; Cornet,S.; Rolland,A.; Marin,J.-G.; Bigg,D.; Chabrier,P.-E.
参考来源:Bioorg Med Chem Lett 2004,14(1),157
产品链接: CAS No. 335242-75-6››