Palladium-catalyzed asymmetric Heck/carbonyl cyclization--Synthesis and application of various chiral oxidized indole rings
2019-06-14916The team led by PI Zhu Qiang and associate researcher Luo Shuang of the laboratory had successfully conducted the palladium-catalyzed asymmetric Heck/carbonyl cyclization reaction, and the related results were published in Angew. Chem. Int. Ed. (IF 12.102). In this reaction, various indole rings γ- and δ-lactone/lactam are obtained in high yield under mild reaction conditions, which have good enantioselectivity (up to 99% ee). The absolute configuration of the relevant compound was confirmed through single crystal X-ray diffraction. Asymmetric synthesis of potent CRTH2 receptor antagonists has also been demonstrated using this approach in key steps.