Tomelukast, LY-171883
油酸三乙醇胺Chemical Name: 1-[2-Hydroxy-3-propyl-4-[4-(1H-tetrazol-5-yl)butoxy]phenyl]ethanone; 5-[4-(4-Acetyl-3-hydroxy-2-propylphenoxy)butyl]tetrazole
CAS No. 88107-10-2
项目整合开发状态: Phase III
项目研究机构: Lilly (Originator)
合成路线:The condensation of 2,4-dihydroxy-3-prop ylacetophenone (I) with 1 4-dibromobutane (II) by means of K2CO3 in refluxing acetone gives 4-(4 acetyl 3-hydroxy-2-propylphenoxy)butyl bromide (III),which is treated with NaCN in hot DMF to yield 5-(4 acetyl-3-hydroxy-2-propylphenoxy)pen tanenitrile (IV).Finally,this compound is cyclized with sodium azide by means of NH4Cl in DMF at 125 C.
📌 参考资料/链接：
参考文献标题:Leukotriene antagonists
文献作者:Marshall,W.S.; Verge,J.P.(Eli Lilly and Company)
参考来源:EP 0108592
📄 详细内容
合成路线:The condensation of 2,4-dihydroxy-3-prop ylacetophenone (I) with 1 4-dibromobutane (II) by means of K2CO3 in refluxing acetone gives 4-(4 acetyl 3-hydroxy-2-propylphenoxy)butyl bromide (III),which is treated with NaCN in hot DMF to yield 5-(4 acetyl-3-hydroxy-2-propylphenoxy)pen tanenitrile (IV).Finally,this compound is cyclized with sodium azide by means of NH4Cl in DMF at 125 C.
参考文献标题:LY-171883
文献作者:Chu,S.S.
参考来源:Drugs Fut 1985,10(8),632
产品链接: CAS No. 88107-10-2››