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Dr. Guoqin Xia received his B. Sc. Degree from Wuhan University in 2009 and Ph. D. Degree from Shanghai Institute of Organic Chemistry, CAS in 2014. His project was focused on Palladium (II)-catalyzed tandem cyclization reactions during his doctoral training under the supervision of Prof. Xiyan Lu. In 2015, Dr. Xia joined Prof. Jin-Quan Yu’s group at Scripps Research as a Research Associate, during which he studied site- and stereo-selective C(sp³)-H activation. In 2018, he joined Prof. Stuart L. Schreiber’s group as a Research Associate and developed many novel aza-spiro-skeletons which could be used in DNA-encoded chemical library synthesis. Dr. Guoqin Xia is now a Principal Investigator at Shanghai Institute of Materia Medica, CAS & Zhongshan Institute for Drug Discovery.

1. Novel bio-compatible chemical transformations development, including those bond-forming reactions for carboxylic acids, hydroxyl groups, amines etc.

2. Modular asymmetric synthetic methodologies towards multi-cyclic fused heterocycles and screening of these chemical library.

3. Covalent inhibitors design, synthesis and screening for K-Ras mutation proteins.

1. Reactivity and site-selectivity are two major challenges in C(sp³)-H activation. We developed a series of electron-deficient 2-pydone ligands which could significantly enhance the C-H cleavage step and also two different directing groups based on ring-strain to address the site-selectivity for masked alcohol substrates.

2. We developed a series of Pd(II)-catalyzed redox-neutral tandem cyclization reactions and applied these methods in the synthesis of biologically important molecules. The most important finding in these works is that the vinyl carbon-palladium bond generated by aminopalladation or oxypalladation are reactive towards nitrile due to the electronic effect of the heteroatom, which is traditionally not possible in palladium chemistry.

1. Xia, G.; Zhuang, Z.; Liu, L.; Schreiber, S. L.; Melillo, B.; Yu, J.-Q. “Ligand enabled b-methylene C(sp³)-H arylation of masked aliphatic alcohols.” Angew. Chem. Int. Ed. 2020, 59, 7783.  

2. Herron, A.; Liu, D.; Xia, G.; Yu, J.-Q. “δ-C–H mono- and di-halogenation of alcohols” J. Am. Chem. Soc. 2020, 142, 2766.

3. Xia, G.; Weng, J.; Liu, L.; Verma, P.; Li, Z.; Yu, J.-Q. “Reversing conventional site-selectivity in C(sp³)-H bond activation.” Nature Chemistry 2019, 11, 571.

4. Wang, P.; Verma, P.; Xia, G.; Shi, J.; Qiao, J. X.; Tao, S.; Cheng, P. T. W.; Poss, M. A.; Farmer, M. E.; Yeung, K.-S.; Yu, J.-Q. “Ligand-accelerated non-directed C?H functionalization of arenes.” Nature 2017, 551, 489.

5. Jain, P.; Verma, P.; Xia, G.; Yu, J.-Q. “Enantioselective amine α-functionalization via palladium-catalysed C–H arylation of thioamitdes.” Nature Chemistry 2017, 9, 140. 

6. Shen, K.; Han, X.; Xia, G.; Lu, X. “Cationic Pd (II)-Catalyzed Cyclization of N-Tosyl-aniline Tethered Alkynyl Ketones Initiated by Hydropalladation of Alkynes: A Facile Way to 1, 2-Dihydro or 1, 2, 3, 4-Tetrahydroquinoline Derivatives.” Org. Chem. Front. 2015, 2, 145.

7. Xia, G.; Han, X.; Lu, X. “Efficient Synthesis of Heterocyle-Fused β-Naphthylamines via Intramolecular Addition to a Cyano Group Initiated by Nucleopalladation of Alkynes.” Org. Lett. 2014, 16, 6184.

8. Xia, G.; Han, X.; Lu, X. “Pd(II)-Catalyzed One-Step Construction of Cycloalkane-Fused Indoles and Its Application in Formal Synthesis of (±)-Aspidospermidine.” Org. Lett. 2014, 16, 2058.

9. Xia, G.; Han, X.; Lu, X. “Palladium(II)-Catalyzed Tandem Cyclization of 2-(Alk-2’-ynyloxy)benzonitriles or 2-(Alk-2’-ynylamino)- benzonitriles: A Facile Way to 2H-Chromene and 1,2-Dihydroquinoline Derivatives.” Adv. Synth. Catal. 2012, 354, 2701.