一种合成官能化氨基酸的对映选择性方法：抗癫痫药物（R）-拉科酰胺的全合成。
An enantioselective approach to functionalized amino acids: total synthesis of antiepileptic drug (R)-lacosamide.
作者信息
Garg Yuvraj, Pandey Satyendra Kumar
机构信息
School of Chemistry and Biochemistry, Thapar University, Patiala 147001, India.
出版信息
J Org Chem. 2015 Apr 17;80(8):4201-3. doi: 10.1021/acs.joc.5b00480. Epub 2015 Mar 31.
PMID:25798932
Abstract
A short and highly efficient synthetic approach to enantiopure functionalized amino acids (FAAs) 1 skeleton from racemic butadiene monoepoxide as a starting material and its application to the total synthesis of an antiepileptic drug (R)-lacosamide 2 are described. The synthesis utilizes the palladium catalyzed Trost's Dynamic Kinetic Asymmetric Transformation (DYKAT) as key step.
摘要
描述了一种以外消旋丁二烯单环氧化物为起始原料，高效合成对映体纯官能化氨基酸（FAA）1骨架的方法及其在抗癫痫药物（R）-拉科酰胺2全合成中的应用。该合成以钯催化的特罗斯特动态动力学不对称转化（DYKAT）为关键步骤。
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