reaction provides easy access to a wide array of enantiomerically enriched β-fluoropiperidines in good yields and with excellent enantioselectivity. Notably, Et4 NF⋅3 HF as a readily accessible nucleophilic fluoride source was found to play an essential role in the enantioselective control, and CsOCF3 also acts a key additive to improve the excellent ee value of products.
已经开发出使用手性
喹啉-
恶唑啉(Quox)作为
配体的未活化烯烃的第一种不对称PdII催化的
氨基
氟化。该反应可容易地以良好的收率和优异的对映选择性接近大量对映体富集的β-
氟哌啶。值得注意的是,已发现Et4NF⋅3HF作为一种易于获得的亲核
氟化物源,在对映选择性控制中起着至关重要的作用,而CsOCF3也是提高产品ee值的关键添加剂。