Giustiniano Mariateresa, Mercalli Valentina, Cassese Hilde, Di Maro Salvatore, Galli Ubaldina, Novellino Ettore, Tron Gian Cesare
Dipartimento di Farmacia, Università di Napoli "Federico II" , via D. Montesano 49, 80131 Napoli, Italy.
J Org Chem. 2014 Jul 3;79(13):6006-14. doi: 10.1021/jo5005444. Epub 2014 Jun 20.
(Z)-Arylchlorooximes and α-isocyanoacetamides undergo a smooth reaction to produce 1,3-oxazol-2-oxime derivatives in good yields. Opening of the oxazole ring and deoximation reaction give a facile access to aryl-α-ketoamide amides, a class of privileged scaffolds in medicinal chemistry and important synthetic intermediates in organic chemistry.
(Z)-芳基氯肟与α-异氰基乙酰胺能顺利反应,以良好的产率生成1,3-恶唑-2-肟衍生物。恶唑环的开环和脱肟反应能方便地得到芳基-α-酮酰胺酰胺,这是药物化学中的一类特殊骨架以及有机化学中重要的合成中间体。