EGIS-9637

Chemical Name: (?-5-(4-Aminophenyl)-N-cyclopropyl-8-methyl-8,9-dihydro-7H-[1,3]dioxolo[4,5-h][2,3]benzodiazepine-7-carboxamide
CAS No. 220669-66-9
项目整合开发状态: Preclinical
项目研究机构: Egis (Originator)
合成路线:The known 7,8-dihydro-8-methyl-5-(4-nitrophenyl)-9H-1,3-dioxolo-[4,5-h]-2,3-benzodiazepine (I) was condensed with 1,1'-carbonyldiimidazole (II) in refluxing THF to produce imidazolide (III).Subsequent reaction of (III) with boiling cyclopropylamine (IV) gave rise to the cyclopropylcarbamoyl derivative (V).The nitro group of (V) was then reduced to the corresponding amine by hydrogenation over Pd/C.
📌 参考资料/链接:
参考文献标题:1,3-Dioxolo[4,5-h][2,3]benzodiazepine derivs.as AMPA/kainate receptor inhibitors
文献作者:Simig,G.; Sim? A.; Gacs醠yi,I.; Gigler,G.; Szab? G.; Seres,P.; Gyerty醤,I.; Egyed,A.; Szabados,T.; K髏ay Nagy,P.; Kov醕s,A.; Bal醶s,L.; Greff,Z.; L関ay,G.; R醫kai,Z.; V間h,M.; et al.(Egis Pharmaceuticals Ltd.)
参考来源:EP 1015457; WO 9907708