Highly Diastereoselective Synthesis of 4-N-Methylformamidino Trinem (GV129606), a Potent Antibacterial Agent
作者:Stefano Biondi、Angelo Pecunioso、Filippo Busi、Stefania A Contini、Daniele Donati、Micaela Maffeis、Domenica A Pizzi、Luciana Rossi、Tino Rossi、Fabio M Sabbatini
DOI:10.1016/s0040-4020(00)00414-2
日期:2000.7
In this paper a highly diastereoselective synthesis of 4-N-methylformamidino trinem 3 is reported. The route offers advantages compared to that previously used, i.e. the higher overall yield, the robustness, the avoidance of toxic reagents. Most of the compounds were isolated by precipitation, therefore reducing the number of chromatographic separations. The efficient conversion of 4-N-methylamino
在本文中,报道了4- N-甲基甲酰胺基trinem 3的高度非对映选择性合成。与以前使用的路线相比,该路线具有优势,即更高的总收率,坚固性,避免了有毒试剂。大多数化合物通过沉淀分离,因此减少了色谱分离次数。通过使用清除剂树脂的新方法获得了4- N-甲基氨基三苯甲基11到GV129606 3的有效转化。本文提出的途径可以为早期开发研究准备所需的材料,并证明环己烯基氮杂环丁酮12的多功能性 在合成4-取代的triems。