新产品编号:2395657
Chemical Name: 3,5-Dichloro-N-[1(S)-[2-(2-chloropyridin-3-ylamino)-3,4-dioxo-1-cyclobuten-1-ylamino]-2,2-dimethylpropyl]benzamide
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:Condensation between 3-amino-2-chloropyridine (I) and 3,4-diethoxycyclobut-3-ene-1,2-dione (II) in refluxing EtOH affords the (pyridylamino)cyclobutenedione (III).The remaining ethoxy group of (III) is then displaced with methanolic ammonia to furnish the diamino cyclobutenedione (IV).
合成路线:Reaction of 3,5-dichlorobenzamide (V) with pivalaldehyde (VI) in the presence of benzotriazole (VII) gives rise to the benzotriazolyl benzamide (VIII).This is then condensed with the diamino cyclobutene (IV) to afford the racemic adduct (IX),which is finally resolved into the enantiomers employing chiral chromatography.
📌 参考资料/链接：
参考文献标题:Aminal diones as potassium channel openers
文献作者:Basha,F.Z.; Carroll,W.A.; Kort,M.E.; Gregg,R.J.; Dinges,J.; Perez Medrano,A.(Abbott Laboratories Inc.)
参考来源:US 2002165264; US 6495576; WO 0262761
📄 详细内容
合成路线:Reaction of 3,5-dichlorobenzamide (V) with pivalaldehyde (VI) in the presence of benzotriazole (VII) gives rise to the benzotriazolyl benzamide (VIII).This is then condensed with the diamino cyclobutene (IV) to afford the racemic adduct (IX),which is finally resolved into the enantiomers employing chiral chromatography.
参考文献标题:Aminal-containing ATP-sensitive potassium channel openers for the treatment of bladder overactivity
文献作者:Kort,M.E.; Gregg,R.J.; Perez-Medrano,A.; et al.
参考来源:224th ACS Natl Meet (Aug 18 2002,Boston) 2002,Abst MEDI 351