新产品编号:416575

Chemical Name: 2-(5-Amidino-2-hydroxyphenoxy)-6-[3-(1-methyl-4,5-dihydro-1H-imidazol-2-yl)phenoxy]pyridine-4-carboxylic acid bis(trifluoroacetate) monohydrate
CAS No. 213839-78-2 (anhydrous), 213839-59-9 (anhydrous, free base)
项目整合开发状态: Preclinical
项目研究机构: Berlex (Originator)
合成路线:2,6-Dichloropyridine-4-carbonyl chloride (I) is reacted with ethanol and triethylamine to produce the ethyl ester (II).Subsequent displacement of one chloride group of (II) with 5-cyano-2-(benzyloxy)phenol (III) in the presence of Cs2CO3 in DMSO affords the diaryl ether (IV).The remaining chloride group of (IV) is then displaced with the imidazoline phenol (V),yielding the bis(aryloxy) pyridine (VI).Conversion of the cyano group of (VI) into the target amidine is accomplished under standard Pinner conditions.The title compound is finally purified by reversed-phase preparative HPLC in the presence of trifluoroacetic acid,producing the title bis-trifluoroacetate salt.