PNU-109230

Chemical Name: N-[3-[3-Fluoro-4-[4-(2-hydroxy-1-oxoethyl)piperazin-1-yl]phenyl]-2-oxooxazolidin-5(S)-ylmethyl]-2,2-dichloroacetamide
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:Hydrogenolysis of PNU-100542 (I) removed the benzyloxycarbonyl group and afforded secondary amine (II),which was acylated with (acetoxy)acetyl chloride (III) in the presence of triethylamine to provide amide PNU-142581 (IV).Then,acetate and phthaloyl protecting groups were both removed on treatment with an hydroalcoholic solution of methylamine,and the resulting aminoalcohol PNU-141718 (V) was N-acylated with dichloroacetyl chloride (VI) to yield the desired amide PNU-109230.
📌 参考资料/链接:
参考文献标题:Synthesis and biological activity of N-acetyl modified analogs of oxazolidinone anticancer agents linezolid and eperezolid
文献作者:Ulanowicz,D.A.; et al.
参考来源:37th Intersci Conf Antimicrob Agents Chemother (Sept 28-Oct 1,Toronto) 1997,Abst F-21