Yamada Kohei, Kamimura Naoto, Kunishima Munetaka
Faculty of Pharmaceutical Sciences, Institute of Medical, Pharmaceutical, and Health Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan.
Beilstein J Org Chem. 2017 Jul 27;13:1478-1485. doi: 10.3762/bjoc.13.146. eCollection 2017.
A novel method for the synthesis of trisubstituted oxazoles via a one-pot oxazole synthesis/Suzuki-Miyaura coupling sequence has been developed. One-pot formation of 5-(triazinyloxy)oxazoles using carboxylic acids, amino acids and a dehydrative condensing reagent, DMT-MM, followed by Ni-catalyzed Suzuki-Miyaura coupling with boronic acids provided the corresponding 2,4,5-trisubstituted oxazoles in good yields.
一种通过一锅法恶唑合成/铃木-宫浦偶联序列合成三取代恶唑的新方法已被开发出来。使用羧酸、氨基酸和脱水缩合试剂DMT-MM一锅法形成5-(三嗪基氧基)恶唑,然后与硼酸进行镍催化的铃木-宫浦偶联,以良好的产率得到相应的2,4,5-三取代恶唑。