School of Chemistry , University of Bristol , Bristol , BS8 1TS , United Kingdom.
Pharmaceutical Technology & Development , AstraZeneca , Charter Way , Macclesfield , SK10 2NA , United Kingdom.
J Am Chem Soc. 2019 Feb 27;141(8):3356-3360. doi: 10.1021/jacs.8b12689. Epub 2019 Feb 18.
Pd(0)-systems modified with SPINOL-derived phosphoramidate ligands promote highly enantioselective aza-Heck cyclizations of alkenyl N-(tosyloxy)carbamates. The method provides versatile access to challenging N-heterocycles and represents the broadest scope enantioselective aza-Heck protocol developed to date.
SPINOL 衍生的膦酰胺配体修饰的 Pd(0)体系促进了烯基 N-(对甲苯磺酰氧基)氨基甲酸酯的高对映选择性氮杂 Heck 环化反应。该方法为具有挑战性的 N-杂环化合物提供了通用的合成途径,代表了迄今为止开发的最广泛的对映选择性氮杂 Heck 反应协议。