SCH-60663

4-[(2S,3R)-1-(4-氟苯基)-3-[(3S)-3-(4-氟苯基)-3-羟基丙基]-4-氧代-2-氮杂环丁基]苯基beta-D-吡喃葡糖苷酸Chemical Name: 1-O-[4-[(2S,3R)-1-(4-Fluorophenyl)-3-[3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4-oxo-2-azetidinyl]phenyl]-beta-D-glucopyranosiduronic acid
CAS No. 190448-57-8
项目整合开发状态: Preclinical
项目研究机构: Schering-Plough (Originator)
合成路线:Protected glucuronic acid (I) was converted to trichloroacetimidate (II) by treatment with trichloroacetonitrile and Cs2CO3.

合成路线:Diol (III) was acetylated with Ac2O in the presence of dimethylaminopyridine to yield diester (IV),which was selectively hydrolyzed to monoacetate (V) by means of methanolic guanidine.Coupling of phenol (V) with imidate (II) by means of boron trifluoride etherate furnished the protected glucuronide (VI).The ester groups of (VI) were finally hydrolyzed by treatment with triethylamine in aqueous methanol.