Shanghai Institute of Material Medical Chinese Academy of Sciences

Biography

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.

Education

2009.09-2014.06 Shanghai Institute of Organic Chemistry，Ph. D. of Organic Chemistry

2005.09-2009.06 Wuhan University，B. Sc. of Applied Chemistry

Work Experience

1.2021.06 to Present Principal Investigator, Shanghai Institute of Materia Medica & Zhongshan Institute for Drug Discovery

2.2020.10-2021.04 Staff Scientist, The Scripps Research Institute，Benjamin F. Cravatt group

3.2018.03-2020.10 Research Associate, The Scripps Research Institute & Broad Institute，Stuart L. Schreiber group

4.2015.10-2018.03 Research Associate, The Scripps Research Institute，Jin-Quan Yu group

5.2014.06-2015.10 Research Assistant, Shanghai Institute of Organic Chemistry, Xiyan Lu group

Research Directions

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.

Grants & Research Projects

Achievements

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.

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Social Titles

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Awards & Honors

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Pubilcations

Selected Publications

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

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.*Highlighted by C&E News, Synfacts, X-MOL and CBG chemistry blogs

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.

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