NO-Ursodeoxycholic acid, NO-UDCA, NCX-1000

Chemical Name: (3alpha,5beta,7beta)-3,7-Dihydroxycholan-24-oic acid 2-methoxy-4-[3-[4-(nitrooxy)butoxy]-3-oxo-1(E)-propenyl]phenyl ester
CAS No. 301828-26-2
项目整合开发状态: Phase I
项目研究机构: NicOx (Originator), Axcan (Licensee)
合成路线:Ferulic acid (I) was converted to the 4-bromobutyl ester (II) upon treatment with carbon tetrabromide,triphenylphosphine and THF also as the solvent.Coupling of dihydroxycholanoic acid (III) with ferulic acid bromobutyl ester (II) using DCC in the presence of DMAP furnished diester (IV).Finally,displacement of the bromide group of (IV) with silver nitrate gave rise to the title nitrooxy derivative.