Fidexaban, ZK-807834, BX-807834, ZK-807191(diHCl), PD-200022, CI-1031

合成路线:ZK-807834 is obtained by condensation of the diaryl ether (I) with the phenol (II) by means of K2CO3 to afford the bisaryl ether (III).Reaction of the cyano group of (III),first with HCl in ethanol and then with ammonia,yields the corresponding amidino compound (IV),which is finally demethylated with HBr.

合成路线:Coupling of 4-methyl-2,3,5,6-tetrafluoropyridine (I) with two molecules of 3-hydroxybenzonitrile (II) in the presence of NaH in hot DMF produced the 2,6-bis(phenoxy)pyridine (III).Conversion of the nitrile groups of (III) into the target bisamidine was then achieved by formation of the corresponding imidate (IV) with ethanol and HCl,followed by treatment with ethanolic ammonia at 60 C in a sealed tube.

参考文献标题:Discovery of N-[2-[5-[amino(imino)methyl]-2-hydroxyphenoxy]-3,5-difluoro-6-[3-(4,5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylglycine (ZK-807834): A potent,selective,and orally active inhibitor of the blood coagulation enzyme factor
文献作者:Phillips,G.B.; Buckman,B.O.; Davey,D.D.; Eagen,K.A.; Guilford,W.J.; Hinchman,J.; Ho,E.; Koovakkat,S.; Liang,A.; Light,D.R.; Mohan,R.; Ng,H.P.; Post,J.M.; Shaw,K.J.; Smith,D.; Subramanyam,B.; Sullivan,M.E.; Trinh,L.; Vergona,R.; et al.
参考来源:J Med Chem 1998,41(19),3557


合成路线:ZK-807834 is obtained by condensation of the diaryl ether (I) with the phenol (II) by means of K2CO3 to afford the bisaryl ether (III).Reaction of the cyano group of (III),first with HCl in ethanol and then with ammonia,yields the corresponding amidino compound (IV),which is finally demethylated with HBr.
参考文献标题:ZK-807834
文献作者:Ricart-Diaz,M.; Castar,J.
参考来源:Drugs Fut 2002,27(8),748


产品链接: CAS No. 183305-24-0››