EGIS-8465(free base), EGIS-9933
Chemical Name: 5-(2-Methoxybenzyl)-2-[2-[4-[3-(trifluoromethyl)benzyl]piperazin-1-yl]ethylsulfanyl]pyrimidine-4,6-diamine hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Egis (Originator), Servier (Licensee)
合成路线:EGIS-9933 was synthesized by S-alkylation of 4,6-diamino-2-mercapto-5-(2-methoxybenzyl)pyrimidine (I) with 1-(2-chloroethyl)-4-[3-(trifluoromethyl)benzyl]piperazine (II) in the presence of potassium carbonate and a catalytic amount of potassium iodide in refluxing methanol.The product was recrystallized from aqueous ethanol,and converted to the hydrochloride.
📌 参考资料/链接：
参考文献标题:Novel piperazinylalkylthiopyrimidine derivs.,pharmaceutical compsns.containing the same and a process for the preparation of the novel cpds.
文献作者:Jak骳zi,I.; B髗sing,D.; R醫zn?Simonek,I.; Gacs醠yi,I.; Sz閚醩i,G.; Schmidt,E.; Mikl髎n?Kov醕s,A.; Bilkei Gorz? A.; Blask? G.; Gyerty�? I.; N閙eth,G.; Simig,G.; Tihanyi,K.; Egyed,A.(Egis Pharmaceuticals Ltd.)
参考来源:EP 0901473; JP 1999514641; WO 9716429