手性催化剂促进的 α-芳基 α-腙酯和酰胺的对映选择性合成。
Catalytic enantioselective synthesis of α-aryl α-hydrazino esters and amides.
机构信息
Departamento de Química Orgánica, Universidad de Sevilla and Centro de Innovación en Química Avanzada (ORFEO-CINQA), C/Prof. García González, 1, 41012 Sevilla, Spain.
出版信息
Chem Commun (Camb). 2020 May 28;56(43):5823-5826. doi: 10.1039/d0cc02478c. Epub 2020 Apr 24.
Catalysts generated by combinations of Pd(TFA) and pyridine-hydrazone ligands have allowed the asymmetric 1,2-addition of aryl boronic acids to N-carbamoyl (Cbz and Fmoc) protected glyoxylate-derived hydrazones, yielding α-aryl α-hydrazino esters/amides in high enantioselectivities. Subsequent removal of the carbamoyl moiety affords key building blocks en route to hydrazinopeptides, N-aminopeptides and peptidomimetics thereof.
钯（TFA）和吡啶-腙配体组合生成的催化剂允许芳基硼酸对 N-碳酰胺（Cbz 和 Fmoc）保护的乙醛酸衍生腙进行不对称 1,2-加成，生成高对映选择性的α-芳基α-酰肼基酯/酰胺。随后去除碳酰胺部分可得到通往酰肼肽、N-氨基肽及其肽类似物的关键构建块。
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