Wy-49051
Chemical Name: 7-[3-[4-(Diphenylmethoxy)-1-piperidinyl]propyl]-3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione fumarate hemihydrate; 7-[3-[4-(Diphenylmethoxy)piperidino]propyl]theophylline fumarate hemihydrate
CAS No. 113418-60-3
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:Reaction of theophylline (I) with 1,3-dibromopropane (II) in DMF in the presence of triethylamine afforded the bromo intermediate (III)) in 77% yield.Reaction of (III) with 4-hydroxypiperidine (IV) in DMF in the presence of sodium bicarbonate afforded the unsubstituted hydroxypiperidinyl intermediate (V) in 31% yield which was subsequently alkylated with diphenylmethylbromide (VI) to afford Wy-49,051 in 29% yield.
📌 参考资料/链接：
参考文献标题:Histamine H1-antagonists
文献作者:Abou-Gharbia,M.A.; Nielsen,S.T.; Webb,M.B.(American Home Products Corp.)
参考来源:EP 0271192; GB 2196963; JP 1988152381; US 4716166
📄 详细内容
合成路线:Reaction of theophylline (I) with 1,3-dibromopropane (II) in DMF in the presence of triethylamine afforded the bromo intermediate (III)) in 77% yield.Reaction of (III) with 4-hydroxypiperidine (IV) in DMF in the presence of sodium bicarbonate afforded the unsubstituted hydroxypiperidinyl intermediate (V) in 31% yield which was subsequently alkylated with diphenylmethylbromide (VI) to afford Wy-49,051 in 29% yield.
参考文献标题:Wy-49,051
文献作者:Abou-Gharbia,M.
参考来源:Drugs Fut 1990,15(2),137