Ligand-Enabled Stereoselective β-C(sp(3))-H Fluorination: Synthesis of Unnatural Enantiopure anti-β-Fluoro-α-amino Acids.
Ligand-Enabled Stereoselective β-C(sp(3))-H Fluorination: Synthesis of Unnatural Enantiopure anti-β-Fluoro-α-amino Acids.
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DOI：
10.1021/jacs.5b04088
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发表时间：
2015-06-10
影响因子：
15
通讯作者：
Yu JQ
中科院分区：
文献类型：
--
作者：
Zhu RY;Tanaka K;Li GC;He J;Fu HY;Li SH;Yu JQ
首次发现喹啉类配体对钯催化的β-C（sp3）-氢键有促进作用。以L-丙氨酸为原料，通过β-C（sp ~ 3）-H芳基化和立体选择性取代，合成了一系列非天然对映体纯的含氟α-氨基酸。
A quinoline-based ligand was shown to promote palladium-catalyzed β-C(sp3)–H fluorination for the first time. A range of unnatural enantiopure fluorinated α-amino acids were obtained through sequential β-C(sp3)–H arylation and subsequent stereoselective fluorination from readily available L-alanine.