Kobe Pharmaceutical University, Motoyamakita, Higashinada, Kobe, Hyogo 658-8558, Japan.
Org Lett. 2011 Feb 4;13(3):518-21. doi: 10.1021/ol1029035. Epub 2010 Dec 28.
A regioselective intramolecular cyclization/halogenation reaction of N-alkoxy-o-alkynylbenzamides with CuCl(2)/NCS was developed. The corresponding 3-(chloromethylene)isobenzofuran-1-ones were exclusively obtained via 5-exo-dig cyclization in moderate to excellent yields within 0.5-1 h. This approach has been successfully used to synthesize a biaryl compound by the Suzuki-Miyaura reaction.
一种 N-烷氧基-O-炔基苯甲酰胺与 CuCl(2)/NCS 的区域选择性分子内环化/卤化反应被开发出来。通过 5-endo-dig 环化,在 0.5-1 小时内以中等至优异的收率得到了相应的 3-(氯亚甲基)异苯并呋喃-1-酮。该方法已成功地通过Suzuki-Miyaura 反应合成了一种联苯化合物。