新产品编号:801001

Chemical Name: 2(R)-(Methylamino)-3-(4-phenoxyphenylsulfonyl)propionohydroxamic acid
CAS No. 310464-35-8 (enantiomer)
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:The reaction of N-(benzyloxycarbonyl)-L-serine methyl ester (I) with Ts-Cl gives the corresponding tosylate (II),which is condensed with 4-phenoxythiophenol (III) to yield the thioether (IV).The oxidation of (IV) with Oxone affords the sulfone (V),which is N-deprotected with H2 over Pd/C to provide compound (VI) with a free amino group.The methylation of (VI) with methyl iodide gives the N-methyl derivative (VII),which is finally treated with hydroxylamine to afford the target hydroxamic acid.
📌 参考资料/链接:
参考文献标题:alpha-Amino-beta-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1
文献作者:Becker,D.P.; Barta,T.E.; Bedell,L.; DeCrescenzo,G..; Freskos,J.N.; Getman,D.P.; Hockerman,S.L.; Li,M.; Mehta,P.; Mischke,B.V.; Munie,G.E.; Swearingen,C.; Villamil,C.I.
参考来源:Bioorg Med Chem Lett 2001,11(20),2719