NS-8
2-氨基-5-(2-氟苯基)-4-甲基-1H-吡咯-3-碳酈Chemical Name: 2-Amino-5-(2-fluorophenyl)-4-methyl-1H-pyrrole-3-carbonitrile
CAS No. 186033-14-7
项目整合开发状态: Phase II
项目研究机构: Nippon Shinyaku (Originator), Apogepha (Licensee)
合成路线:Treatment of 2-fluorophenylglycine (I) with Ac2O and pyridine at 150 C produced 1-(2-fluorophenyl)-1-acetamido-2-propanone (II).This was subsequently condensed with malononitrile yielding the title pyrrole derivative.
📌 参考资料/链接：
参考文献标题:Pyrrole derivs.and medicinal compsn.
文献作者:Tsuda,M.; Tanaka,M.; Nakamura,A.(Nippon Shinyaku Co.,Ltd.)
参考来源:US 5998459; WO 9640634
📄 详细内容
合成路线:The partial hydrolysis of malonodinitrile (I) with HCl in ethanol gives 2-cyanoacetamide (II),which is treated with ammonia in ethanol to yield 3,3-diaminopropenenitrile (III).Finally,this compound is cyclized with 2-bromo-1-(2-fluorophenyl)-1-propanone (IV) by means of TEA in ethanol.
参考文献标题:Studies on potassium channel openers: Synthesis and pharmacological properties of novel pyrrole derivatives
文献作者:Tsuda,M.; et al.
参考来源:20th Symp Med Chem (Dec 6 2000,Tokyo) 2000,Abst 2P-24
产品链接: CAS No. 186033-14-7››