Lee Sung-Chan, Park Seung Bum
Department of Chemistry, Seoul National University, Seoul 151-747, Korea.
J Comb Chem. 2007 Sep-Oct;9(5):828-35. doi: 10.1021/cc0700492. Epub 2007 Jun 26.
A practical solid-phase strategy for the synthesis of Delta(5)-2-oxopiperazines via N-acyliminium ion cyclization has been developed. A key step in the library synthesis is tandem acidolytic cleavage with subsequent in situ iminium formation, followed by stable enamide transformation. This approach is exemplified by the preparation of a 192-member pilot library using bromoacetal resins without further purification.
已经开发出一种通过N-酰基亚胺离子环化合成δ(5)-2-氧代哌嗪的实用固相策略。文库合成中的关键步骤是酸解裂解并随后原位形成亚胺离子，接着进行稳定的烯酰胺转化。使用溴代缩醛树脂制备一个192个成员的先导文库，无需进一步纯化，以此为例说明了该方法。
