School of Chemistry & Chemical Engineering, Yangzhou University, Yangzhou, Jiangsu 225002, China.
Org Lett. 2023 Jun 30;25(25):4682-4687. doi: 10.1021/acs.orglett.3c01561. Epub 2023 Jun 19.
A highly efficient Pd-catalyzed carboetherification reaction of β,γ-unsaturated ketoximes with propargylic acetates is demonstrated. This method provides a practical protocol for accessing the incorporation of an allene moiety into 3,5-disubstituted and 3,5,5-trisubstituted isoxazolines. The salient features of this transformation include a broad substrate scope, good functional group tolerance, an easy scale-up, versatile transformations, and applications in the late-stage modification of drugs.
本文报道了钯催化的β,γ-不饱和酮肟与丙炔酸酯的高立体选择性的碳醚化反应。该方法为烯丙基片段引入 3,5-二取代和 3,5,5-三取代异恶唑啉提供了一种实用的方案。该转化的突出特点包括广泛的底物范围、良好的官能团耐受性、易于规模化、多功能转化以及在药物后期修饰中的应用。
