Multi-component assembly of the bicyclic core associated with the tRNA synthetase inhibitors SB-203207 and SB-203208. Application to the synthesis of biologically active analogues
Multi-component assembly of the bicyclic core associated with the tRNA synthetase inhibitors SB-203207 and SB-203208. Application to the synthesis of biologically active analogues
复制标题
DOI：
10.1039/b104890m
复制
发表时间：
2001-01-01
影响因子：
4.9
通讯作者：
Yue, WM
中科院分区：
文献类型：
--
作者：
Banwell, MG;Crasto, CF;Yue, WM
酮（+/-）-5，其包含与标题tRNA合成酶抑制剂1和2相关的双环核心，已经通过涉及2-（羟甲基）环庚-2-烯酮（15）、甲胺（6）和丙炔酰胺（10）;容易衍生的乙酸酯（±）-21和（+）-21的直接制备分别提供了标题化合物的生物活性类似物23和24。
The ketone (+/-)- 5, which embodies the bicyclic core associated with the title tRNA synthetase inhibitors 1 and 2, has been prepared via a three-component coupling reaction involving 2-( hydroxymethyl) cyclopent-2-enone (15), methylamine (6) and propiolamide (10); straightforward elaboration of the readily derived acetates ()- 21 and (+)- 21 has provided the biologically active analogues 23 and 24, respectively, of the title compounds.