用于双位点拟肽的β-内酰胺支架的合成。
Synthesis of beta-lactam scaffolds for ditopic peptidomimetics.
作者信息
Palomo Claudio, Aizpurua Jesus M, Balentova Eva, Jimenez Azucena, Oyarbide Joseba, Fratila Raluca M, Miranda José Ignacio
机构信息
Departamento de Química OrgAnica-I, Universidad del País Vasco, Facultad de Química, Apdo 1072, 20080 San SebastiAn, Spain.
出版信息
Org Lett. 2007 Jan 4;9(1):101-4. doi: 10.1021/ol0626241.
[reaction: see text] Ring opening of alpha-substituted-alpha-methoxycarbonyl-N-nosylaziridines provides a practical access to enantiopure alpha,alpha'-disubstituted beta-lactam scaffolds, novel types of ditopic reverse turn surrogates. The procedure is general, short, and high yielding and starts from handy alpha-substituted serinates and alpha-amino acid derivatives.
[反应：见正文] α-取代-α-甲氧基羰基-N-硝酰基氮杂环丙烷的开环反应为对映体纯的α,α'-二取代β-内酰胺骨架（新型双位点反向转角替代物）提供了一条实用的合成途径。该方法具有通用性、步骤简短且产率高，起始原料为便于使用的α-取代丝氨酸酯和α-氨基酸衍生物。
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