Heterocycles from Ylides. Part XI. Synthesis of 2-Substituted Quinoline Derivatives
作者:Piero Dalla Croce、Giuseppe Cremonesi、Francesco Fontana、Concetta La Rosa
DOI:10.3987/com-07-s(w)78
日期:——
2-N-phenylsulfonylaminobenzaldehyde (1) with stabilized alkylidene phosphoranes (2) gives, through a Wittig condensation followed by reduction of intermediate alkenes and cyclization with PPA, quinoline derivatives (5).
A highly diastereoselective method for the synthesis of novel spiro-tetrahydroquinoline derivatives is reported here, using a one-pot reaction method. All compounds were characterized by 1H-nuclear magnetic resonance (NMR) and mass spectroscopy, and their stereo configurations were confirmed by X-ray analysis. These activities of these derivatives were then tested in human keratocyte cells. The responses
本文报道了一种使用一锅反应法合成新型螺-四氢喹啉衍生物的高度非对映选择性方法。所有化合物均通过1 H-核磁共振 (NMR) 和质谱进行表征,并通过 X 射线分析确认其立体构型。然后在人角膜细胞中测试这些衍生物的这些活性。使用划痕分析研究了细胞对选定化合物处理的反应,并在小鼠切除伤口模型中测试了这些化合物。其中三种衍生物表现出显着的伤口愈合活性。