Merck Research Laboratories, Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065-0900, USA.
Org Lett. 2010 Aug 20;12(16):3614-7. doi: 10.1021/ol101346w.
An expedient method for the direct conversion of aldehydes to 2,4-disubstituted oxazoles is presented. The method relies on the oxidation of an oxazolidine formed from the condensation of serine with an aldehyde and proceeds through a 2,5-dihydrooxazole intermediate. In contrast to standard methods that start from carboxylic acids, the use of aldehydes as starting materials does not require intermediate purification and affords the oxazoles under relatively mild conditions.
本文介绍了一种将醛直接转化为 2,4-二取代恶唑的简便方法。该方法依赖于丝氨酸与醛缩合形成的恶唑啉的氧化,并且通过 2,5-二氢恶唑中间体进行反应。与从羧酸开始的标准方法相比,使用醛作为起始原料不需要中间纯化,并且在相对温和的条件下得到恶唑。