新产品编号:1389505
Chemical Name: endo-(5R,6S)-6-[4-(3-Phenyl-2-propynylsulfanyl)-1,2,5-thiadiazol-3-yl]-1-azabicyclo[3.2.1]octane L-(+)-tartrate
项目整合开发状态: Biological Testing
项目研究机构: Novo Nordisk (Originator), Lilly (Codevelopment)
合成路线:Treatment of endo-(+)-3-(3-propylsulfonyl-1,2,5-thiadiazol-4-yl)-1-azabicyclo[2.2.1]heptane (I) with sodium hydrosulfide in hot DMF afforded the intermediate thiol (II),which was further condensed with 3-phenyl-2-propyn-1-yl mesylate (III) to yield the corresponding thioether.This compound was finally isolated as the tartrate salt.
📌 参考资料/链接：
参考文献标题:Heterocyclic cpds.and their preparation and use
文献作者:Sauerberg,P.; Jeppesen,L.(Novo Nordisk A/S)
参考来源:EP 0977755; US 6015813; WO 9847900
📄 详细内容
合成路线:Treatment of endo-(+)-3-(3-propylsulfonyl-1,2,5-thiadiazol-4-yl)-1-azabicyclo[2.2.1]heptane (I) with sodium hydrosulfide in hot DMF afforded the intermediate thiol (II),which was further condensed with 3-phenyl-2-propyn-1-yl mesylate (III) to yield the corresponding thioether.This compound was finally isolated as the tartrate salt.
参考文献标题:Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic M1 receptor activation
文献作者:Sauerberg,P.; Jeppesen,L.; Olesen,P.H.; Sheardown,M.J.; Fink-Jensen,A.; Rasmussen,T.; Rimvall,K.; Shannon,H.E.; Bymaster,F.P.; DeLapp,N.W.; Calligaro,D.O.; Ward,J.S.; Whitesitt,C.A.; Thomsen,C.
参考来源:Bioorg Med Chem Lett 1998,8(20),2897