CAS: 5734-67-8; 4-Chloro-6-Ethylpyrimidin-2-Amine

相似化合物

73576-33-7 5600-21-5 139296-65-4

上下游产品

CAS号5734-66-7 2-氨基-4-羟基-6-乙基嘧啶 | CAS号30414-53-0 丙酰乙酸甲酯 | CAS号58-14-0 乙胺嘧啶 | CAS号514854-12-7 2,4-二氨基-6-乙基嘧啶 | CAS号514854-13-8 6-乙基-5-碘嘧啶-2,4-二胺 | CAS号514854-15-0 2-Pyrimidinamin...

📜3-氧代戊酸甲酯置于potassium Tert-Butylate,四乙基氯化铵,N,N-二甲基苯胺,三氯氧磷体系中,用 甲醇,乙腈 作为反应溶剂,化学反应 0.33H,反应生成 2-氨基-4-氯-6-乙基嘧啶
参考文献:Discovery And Sar Of 6-Alkyl-2,4-Diaminopyrimidines As Histamine H4 Receptor Antagonists
标题:Discovery And Sar Of 6-Alkyl-2,4-Diaminopyrimidines As Histamine H4 Receptor Antagonists
摘要:This Report Discloses The Discovery And Sar Of A Series Of 6-Alkyl-2-Aminopyrimidine Derived Histamine H4 Antagonists That Led To The Development Of Jnj 39758979,Which Has Been Studied In Phase Ii Clinical Trials In Asthma And Atopic Dermatitis. Building On Our Sar Studies Of Saturated Derivatives From The Indole Carboxamide Series,Typified By Jnj 7777120,And Incorporating Knowledge From The Tricyclic Pyrimidines Led Us To The 6-Alkyl-2,4-Diaminopyrimidine Series. A Focused Medicinal Chemistry Effort Delivered Several 6-Alkyl-2,4-Diaminopyrimidines That Behaved As Antagonists At Both The Human And Rodent H4 Receptor. Further Optimization Led To A Panel Of Antagonists That Were Profiled In Animal Models Of Inflammatory Disease. On The Basis Of The Preclinical Profile And Efficacy In Several Animal Models,Jnj 39758979 Was Selected As A Clinical Candidate; However,Further Development Was Halted During Phase Ii Because Of The Observation Of Drug-Induced Agranulocytosis (Diag) In Two Subjects.
DOI:10.1021/jm401727M