Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
Org Lett. 2010 Aug 6;12(15):3456-9. doi: 10.1021/ol1012789.
A novel 2-step synthesis of oxazole-4-carboxylates from aldehydes was developed, which is characterized by the utilization of 3-oxazoline-4-carboxylates as synthetic intermediates. The facile preparation of 4-keto-oxazole derivatives from 3-oxazoline-4-carboxylates based on their interesting reactivity toward Grignard reagents is also described.
开发了一种新颖的两步法从醛制备恶唑-4-羧酸酯的方法,其特点是利用 3-恶唑啉-4-羧酸酯作为合成中间体。还描述了基于 3-恶唑啉-4-羧酸酯对格氏试剂的有趣反应性,从 3-恶唑啉-4-羧酸酯中简便制备 4-酮恶唑衍生物。