Stones Graham, Argouarch Gilles, Kennedy Alan R, Sherrington David C, Gibson Colin L
Department of Pure & Applied Chemistry, University of Strathclyde, 295 Cathedral Street, Glasgow, UK G1 1XL.
Org Biomol Chem. 2003 Jul 7;1(13):2357-63. doi: 10.1039/b302887a.
Using L-valine methyl ester hydrochloride as starting material, the synthesis of (2S)-2-isopropyl-1,4,7-trimethyl-1,4,7-triazacyclononane is described. Various standard Richman-Atkins cyclisation methods gave only poor yields in the key macrocyclisation step. Efficient macrocyclisation yields were, however, realised when an in situ sequential cyclisation method was developed.
以L-缬氨酸甲酯盐酸盐为起始原料，描述了(2S)-2-异丙基-1,4,7-三甲基-1,4,7-三氮杂环壬烷的合成。在关键的大环化步骤中，各种标准的Richman-Atkins环化方法产率都很低。然而，当开发出原位顺序环化方法时，实现了高效的大环化产率。
