Bose D Subhas, Idrees Mohd, Jakka N M, Rao J Venkateswara
Organic Chemistry Division-III, Indian Institute of Chemical Technology, Tarnaka, Hyderabad, India.
J Comb Chem. 2010 Jan-Feb;12(1):100-10. doi: 10.1021/cc900129t.
An efficient and practical method has been manifested for the diversity-oriented synthesis of quinolines via Friedländer annulation reaction for the generation of a wide range of structurally interesting and pharmacologically significant compounds by using ceric ammonium nitrate as a catalyst (10 mol %) at ambient temperature in 45 min. A variety of functional groups are introduced at various positions of the quinoline moiety, and further the diversity of the core skeleton was expanded at R(1) and R(2) positions by the synthesis of various hybrids. Initial screening of the compounds for cytotoxicity against a series of cancer cell lines showed promising results.
一种高效实用的方法已被证明，可通过Friedländer环化反应进行喹啉的多样性导向合成，在室温下以硝酸铈铵为催化剂（10 mol%），45分钟内生成一系列结构有趣且具有药理学意义的化合物。喹啉部分的各个位置引入了多种官能团，并且通过合成各种杂化物进一步扩展了R(1)和R(2)位置核心骨架的多样性。对一系列癌细胞系进行细胞毒性的化合物初步筛选显示出有前景的结果。
