IDR-16084, GYKI-16084, Uroflux
Chemical Name: (+)-(R)-2-[3-(Benzo-1,4-dioxan-2-ylmethylamino)propyl]pyridazin-3(2H)-one hydrochloride
CAS No. 185739-21-3 (free base)
项目整合开发状态: Phase II
项目研究机构: Gedeon Richter (Originator), Ivax (Originator)
合成路线:The enantiomerically pure benzodioxane derivative (VIII) was obtained in a straightforward route including five steps starting from pyrocatechin (I).Racemic (VI) was then resolved by means of crystallization with (-)-O,O'-dibenzoyl-L-tartaric acid.
合成路线:The pyridazinone intermediate (XII) was prepared from dihydroxypyridazine (IX) in three synthetic steps.
合成路线:Finally,N-alkylation of the potassium salt of (XII) with the base form of (VIII) was performed in dimethyl sulfoxide to afford GYKI-16084.
📌 参考资料/链接：
参考文献标题:3(2H)-Pyridazinone derivs.and pharmaceutical compsns.containing these cpds.
文献作者:Horv醫h,E.; Simay,A.; Tomori,?; Druga,A.; Kasztreiner,E.; Tilahun,Y.; Makk,N.; Kir醠y,I.; Kos醨y,J.; Papp,?; Varga,M.; Z醨a,E.; Karim,M.; Sebesty閚,L.; Varga,I.; Bidl? M.; Horv醫h,K.; M醫h? I.; et al.(Gyogyszerkutato Intezet Kft.)
参考来源:WO 9638441
📄 详细内容
合成路线:The enantiomerically pure benzodioxane derivative (VIII) was obtained in a straightforward route including five steps starting from pyrocatechin (I).Racemic (VI) was then resolved by means of crystallization with (-)-O,O'-dibenzoyl-L-tartaric acid.
合成路线:The pyridazinone intermediate (XII) was prepared from dihydroxypyridazine (IX) in three synthetic steps.
合成路线:Finally,N-alkylation of the potassium salt of (XII) with the base form of (VIII) was performed in dimethyl sulfoxide to afford GYKI-16084.
参考文献标题:GYKI-16084
文献作者:M醫yus,P.
参考来源:Drugs Fut 1999,24(10),1072