Department Chemie, Ludwig-Maximilians-Universität München, Butenandtstr. 5-13, Haus F, 81377 München, Germany.
J Org Chem. 2011 Aug 19;76(16):6972-8. doi: 10.1021/jo201250n. Epub 2011 Jul 26.
A general method for the synthesis of 2,4,5-trisubstituted thiazoles has been developed. Starting from commercially available 2-bromothiazole, successive metalations using TMPMgCl·LiCl or TMP(2)Zn·2MgCl(2)·2LiCl lead to the corresponding magnesated or zincated thiazoles which readily react with various electrophiles providing highly functionalized thiazoles.
已经开发出一种合成 2,4,5-三取代噻唑的通用方法。从商业上可获得的 2-溴噻唑开始,使用 TMPMgCl·LiCl 或 TMP(2)Zn·2MgCl(2)·2LiCl 进行连续的金属化反应,得到相应的镁化或锌化噻唑,这些噻唑容易与各种亲电试剂反应,提供高度官能化的噻唑。