MDL-104903
Chemical Name: [4S-(4alpha,5beta)]-N-[1(R*)-(4-Benzyl-5-hydroxyoxazolidin-3-ylcarbonyl)-2-methylpropyl]carbamic acid benzyl ester
项目整合开发状态: Preclinical
项目研究机构: Aventis Pharma (Originator)
合成路线:The reaction of benzyloxycarbonyl-L-valyl-L-phenylalanine (I) with paraformaldehyde and TsOH in refluxing benzene gives the oxazolidinone (II),which is reduced with DIBAL in toluene.
📌 参考资料/链接：
参考文献标题:Substd.oxazolidine calpain and/or cathepsin B inhibitors
文献作者:Peet,N.P.; Mehdi,S.; Linnik,M.D.; Angelastro,M.R.; Kim,H.-O.(Aventis Pharmaceuticals,Inc.)
参考来源:EP 0802909; JP 1998512257; WO 9621655
📄 详细内容
合成路线:The reaction of benzyloxycarbonyl-L-valyl-L-phenylalanine (I) with paraformaldehyde and TsOH in refluxing benzene gives the oxazolidinone (II),which is reduced with DIBAL in toluene.
参考文献标题:Hydroxyoxazolidines as alpha-aminoacetaldehyde equivalents: Novel inhibitors of calpain
文献作者:Peet,N.P.; Kim,H.O.; Marquart,A.L.; Angelastro,M.R.; Nieduzak,T.R.; White,J.N.; Friedrich,D.; Flynn,G.A.; Webster,M.E.; Vaz,R.J.; Linnik,M.D.; Koehl,J.R.; Mehdi,S.; Bey,P.; Emary,B.; Hwang,K.K.
参考来源:Bioorg Med Chem Lett 1999,9(16),2365