通过手性非蛋白氨基酸的从头制备，确定一种新型抗疟脂肽的绝对构型和全合成。
Absolute configuration and total synthesis of a novel antimalarial lipopeptide by the de novo preparation of chiral nonproteinogenic amino acids.
机构信息
Department of Chemistry, Faculty of Science, and Medicinal Chemistry Program of the Life Sciences Institute, National University of Singapore, 3 Science Drive 3, Singapore 117543, Singapore.
出版信息
Org Lett. 2012 Mar 16;14(6):1560-3. doi: 10.1021/ol300293a. Epub 2012 Mar 5.
The absolute configuration (via degradation and Marfey's derivatization studies) and the total synthesis of a novel antimalarial lipid-peptide isolated from Streptomyces sp. (IC(50) = 0.8 μM, Plasmodium falciparum 3D7) is disclosed. To this end, versatile stereocontrolled routes to nonproteinogenic amino acids (via catalytic Mannich, Sharpless methods) and enantiomeric trans fatty acids (via Evans alkylation, Kocienski-Julia olefination) have been developed.
从链霉菌（IC（50）= 0.8 μM，恶性疟原虫 3D7）中分离得到一种新型抗疟脂肽，本文披露了其绝对构型（通过降解和马菲衍生化研究）和全合成。为此，开发了多种立体控制非蛋白氨基酸（通过催化曼尼希，Sharpless 方法）和对映体反式脂肪酸（通过 Evans 烷基化，Kocienski-Julia 烯烃化）的路线。
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