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📜2,2-二甲基丙亚胺盐酸,丙二酸二甲酯置于sodium Methylate体系中,用 甲醇,乙醇 用作溶剂,化学反应 19.25H,反应生成2-叔丁基-4,6-二羟基嘧啶
参考文献:Structure−activity Studies On A Series Of A 2-Aminopyrimidine-Containing Histamine H4 Receptor Ligands
标题:Structure−activity Studies On A Series Of A 2-Aminopyrimidine-Containing Histamine H4 Receptor Ligands
摘要:A Series Of 2-Aminopyrimidines Was Synthesized As Ligands Of The Histamine H-4 Receptor (H4R). Working In Part From A Pyrimidine Hit That Was Identified In An Hts Campaign,Sar Studies Were Carried Out To Optimize The Potency,Which Led To Compound 3,4-Tert-Butyl-6-(4-Methylpiperazin-1-yl)Pyrimidin-2-Ylamine. We Further Studied This Compound By Systematically Modifying The Core Pyrimidine Moiety,The Methylpiperazine At Position 4,The Nh2 At Position 2,And Positions 5 And 6 Of The Pyrimidine Ring. The Pyrimidine 6 Position Benefited The Most From This Optimization,Especially In Analogs In Which The 6-Tert-Butyl Was Replaced With Aromatic And Secondary Amine Moieties. The Highlight Of The Optimization Campaign Was Compound 4,4-[2-Amino-6-(4-Methylpiperazin-1-yl)Pyrimidin-4-Yl]Benzonitrile,Which Was Potent In Vitro And Was Active As An Anti-Inflammatory Agent In An Animal Model And Had Antinociceptive Activity In A Pain Model,Which Supports The Potential Of H4R Antagonists In Pain.
Doi:10.1021/jm8005959