| 徐桂清 |
教育与研究经历： 1992.09~1996.06 河南师范大学，化学专业本科 1996.09~1999.06 河南师范大学，有机化学专业硕士 1999.09~~至今 河南师范大学，助教、讲师、副教授、教授 2003.09~2007.06 浙江大学，医学博士 主讲课程： 药物化学，高等药物化学 研究领域与兴趣： 抗肿瘤药物的设计与合成 药物及药物中间体合成工艺研究 近年来主持（参与）的主要科研项目: 1. 横向项目：赤霉酸新工艺级产业化(H2024097)，2024，30万元， 2. 横向项目：赤霉酸发酵、纯化新工艺及产业化研究(H2023008)，2023-2030，155万元。 3. 横向项目：ALKTRK双靶点抑制剂的研发(H2022007)， 2021-2023，70万元。 4. 国家自然科学基金青年基金项目：靶向Toll样受体8的小分子抑制的设计合成、生物学评价及作用机制研究,(21807026)，2019-2021，25万元，参与(第二完成人)。 5. 河南省科技创新杰出青年支持计划项目：强力霉素绿色合成关键技术及产业化研究(164100510015)，2016-2017，30万元。 6. 河南省科技攻关计划项目：盐酸多西环素合成关键技术及产业化研究(152102310312)，2015-2016。 7. 河南省产学研项目：2,6-二氯苯并噁唑合成新工艺研究(142107000025)，2014，52万元。 8. 河南省产学研项目：硫酸氢氯吡格雷合成新技术研究(122107000011)，2012，40万元。 9. 横向项目：有机药物合成研究(201206)，2011，1万元。 10. 河南省教育厅基础研究项目：卡托普利稀土元素配合物的合成、结构表征、性质及生物活性研究(2010B150016)，2010-2012。 11. 河南省科技攻关计划项目：利塞膦酸钠的新工艺研究及产业化(82102330029) ，2008-2009。 近年来发表论文： 1. Ma Y; Ren WF; Song CM; Xu GQ; Kon, DY. Pd-catalyzed asymmetric allylic alkylation of carboxylic acids for the synthesis of chiral butenolidyl ester prodrugs and peptide-drug conjugates, Organic Letters, 2025, 27(4): 13585-13590 2. Zhang DD; Zhao J; Xu GQ; Wang Y; Li Y; Ren HX; Geng JJ; Du Y; Zhan, CC; Yang SN; Liu DF; Gao JJ; Xiong Y; Zhang HY; Li W; Wang W; Wang D; Li B; He, X; Ma CH; Jiang YQ ; Ding QJ. Discovery of imidazo[1,2-b]pyridazine derivatives as potent and highly selective irreversible bruton's tyrosine kinase (BTK) inhibitors, Journal of Medicinal Chemistry, 2025, 68(11): 10897-10929. 3. Gao E; Zhang HY; Guo YJ; Wang X; Mao LF; Peng LZ; Xu GQ; Yao XJ; Li SH; Long HB; Wang T; Wu HD. Design, synthesis and antiproliferative activity studies of novel 1,2,3-triazole-urea hybrids, Drug Design, Development and Therapy, 2025, 19: 9481-9499 4. Bai DC; Zhon, KB; Chang LN; Qiao Y; Wu F; Xu GQ; Chang JB. Nickel-catalyzed regiodivergent hydrosilylation of α-(fluoroalkyl)styrenes without defluorination. Nature Communications, 2024, 15(1): 6360 5. Gao E; Wang,Y; Fan GL; Xu GQ; Wu ZY; Liu ZJ; Liu JC; Mao LF; Hou XX; Li SH. Discovery of gefitinib-1,2,3-triazole derivatives against lung cancer via inducing apoptosis and inhibiting the colony formation, Scientific Reports, 2024, 14(1): 9223 6. Xu GQ; Lv JY; Ding QJ; Ma CH; Jiang YQ; Yu B. Direct C-H alkylation of benzothiadiazoles via organic photoredox catalysis, Journal of Organic Chemistry,2024, 89(4): 2777-2781 7. Xu GQ; Wang Y; Liu KL; Jiang YQ; Zhang XY; Fan XS. Synthesis of unsymmetrical diaryl oxindoles/isoquinolinediones using 2-phenoxy-1H-benzo[d]imidazole as an integrated diarylating reagent, Organic Chemistry Frontiers, 2023, 10(11): 2728-2733 8. Guo YJ; Wang X; Wang ZZ; Mao LF; Wang JH; Peng LZ; Xu GQ. Synthesis and anti-tumor effects of novel pomalidomide derivatives containing urea moieties, Pharmaceuticals, 2023, 15(12): 1479 9. Yang, Y; Lu, B; Xu, GQ; Wang, XM. Overcoming O-H insertion to para-selective C-H functionalization of free phenols: Rh(II)/Xantphos catalyzed geminal difunctionalization of diazo compounds, ACS Central Science, 2022, 8(5): 581-589 10. Ma, CH; Li, QY; Zhao, MH; Fan, GJ; Zhao, J ; Zhang, DD; Yang, SN; Zhang, ST; Gao, DD; Mao, LF; Zhu, L; Li, W; Xu GQ; Jiang, YQ; Ding, QJ. Discovery of 1-amino-1H-imidazole-5-carboxamide derivatives as highly selective, covalent bruton's tyrosine kinase (BTK) inhibitors, Journal of Medicinal Chemistry, 2021, 64(21): 16242-16270 11. Zhang DD; Xu GQ; Zhao J; Wang Y; Wu XF; He X; Li W; Zhang S; Yang SN; Ma CH; Jiang YQ; Ding QJ. Structure-activity relationship investigation for imidazopyrazole-3-carboxamide derivatives as novel selective inhibitors of Bruton's tyrosine kinase, European Journal of Medicinal Chemistry, 2021, 225: 113724 12. Xu GQ; Chen Q; Wu F; Bai DC; Chang JB; Li XW. Rh(III)-Catalyzed chemodivergent coupling of n-phenoxyacetamides and alkylidenecyclopropanes via C-H activation, Organic Letter, 2021, 23(8): 2927-2932 13. Mao LF; Sun G; Zhao J; Xu GQ; Yuan MM; Li YM. Design, synthesis and antitumor activity of icotinib derivatives, Bioorganic Chemistry, 2021, 105: 104421 14. Xu GQ; Wang JH; Zhou YJ; Mao LF. A high-yield and cost-effective synthesis of spirotetramat, Russian Journal of Organic Chemistry, 2020, 56(10): 1775-1778 15. Jiang YQ; Li YY; Yang TT; Shi X; Suo HJ; Zhang WW; Xu GQ; Li W. Design, synthesis, and antilung adenocarcinoma activity research of novel paeonol Schiff base derivatives containing a 1,2,3-triazole moiety, Journal of the Chinese Chemical Society, 2020, 67(1): 165-171 16. Yang TT; Shi X; Guo LB; Gu SH; Zhang WW; Xu GQ; Li W; Jiang YQ. Design, synthesis, and antitumor activity of novel paeonol derivatives containing the 1, 4-benzoxazinone and 1,2,3-triazole moieties, Journal of Chemical Research, 2019, 43(7-8): 241-247 17. Sun B; Chen JW; Ye F; Lu YJ; Xu GQ; Mao LF; Gao Y; Zhang HW; Wang H; Peng LZ. Synthesis and in vitro antibacterial activity of novel naphthyridinone derivatives, ChemistrySelect, 2019, 4(21): 6552-6556 18. Xu GQ; Gao Y; SunB, Peng LZ; Mao LF; Jiang YQ; Ding QJ. A convenient synthesis and biological research of novel 5,6,7,8-tetrahydro-1,6-naphthyridin- 2(1H)-one derivatives hydrochloride as cytotoxic agents. Journal of Heterocyclic Chemistry, 2018, 55(9), 2151-2156 19. Jiang YQ; Wu K; Fan LM; Zhao JL; Yang YQ; Zhang WW; Xu GQ. Cu(OAc)2.H2O/NH2OH.HCl/CH3COONa: A facile and efficient catalyst system for copper-catalyzed azide–alkyne click reactions in water. Journal of the Chinese Chemical Society, 2018, 65, 505-510 20. Xu GQ; Mao S; Mao LF; Jiang YQ; Zhou Y; Shen JX; Dong WP. Study on a new method for synthesis of mirabegron. Journal of Heterocyclic Chemistry, 2017, 54(5): 2703-2707 21. Xu GQ; Zhao JL; Jiang YQ; Zhang P; Li W. Design, synthesis and antifungal activity of novel indole derivatives linked with the 1,2,3-triazole moiety via the CuAAC click reaction. Journal of Chemical Research, 2016, 40: 269-272 22. Xu GQ; Mao S; Mao; LF; Jiang YQ; Zhang P; Li W. Design, synthesis, and antifungal evaluation of novel 1,4-disubstituted 1,2,3-triazoles containing indole framework. Zeitschrift fur Naturforschung Section B, 2016; 71(9)b: 953-958 23. Jiang YQ; He X; Zhang WW; Li XF; Guo N; Zhao YY; Xu GQ; Li W. Metallic copper wire: a simple, clear and reusable catalyst for the CuAAC reaction in supercritical carbon dioxide. RSC Adv., 2015, 5: 73340-73345. 24. Xu GQ; Kong DY; Li W; Xu WJ; Jiang YQ. Synthesis of maleimide derivatives via CuAAC click chemistry and biological evaluation of their antitumor activity against cancer cell lines Journal of Chemical and Pharmaceutical Research, 2014, 6(5): 947-951 25. Jiang YQ; Kong DY; Zhao JL; Qi QH; Li W; Xu GQ. Cu(OAc)2.H2O/NH2NH2.H2O: an efficient catalyst system that in situ generates Cu2O nanoparticles and HOAc for Huisgen click reactions. RSC Advances, 2014, 4: 1010-1014 26. Jiang YQ; Kong DY; Zhao JL; Zhang WW; Xu WJ; Li W , Xu GQ. Simple, efficient thermally promoted protocol for Huisgen-click reaction catalyzed by 10.CuSO4.5H2O in water. Tetrahedron Letter, 2014 (55): 2410–2414 27. Huo RN; Xu GQ; Jiang XY; Ge Y; Xue ZK; Cui FL. Calf thymus DNA binding studies of the new neodymium–naproxen complex. Journal of Biochemical and Molecular Toxicology, 2012, 26(5): 193-198 28. Ye Q; Xu GQ; Lv D; Cheng Z; Li J; Hu YZ. Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3b (GSK-3b) inhibitors. Bioorganic & Medicinal Chemistry. 2009, 17: 4302-4312 29. Xu GQ; He QJ; Yang B; Hu YZ. Synthesis and antitumor activity of novel 4-chloro-3-arylmaleimide derivatives. Letters in Drug Design and Discovery, 2009, 6(1)：51-55 30. 徐桂清; 胡永洲; 张冲; 何俏军; 杨波. 吲哚马来酰亚胺类化合物的合成及其抗肿瘤活性. 有机化学, 2009, 29(6): 916-923 31. Xu GQ; Zhang C; Zhang L; Zhou XL; Yang B; He QJ; Hu YZ. Synthesis, cytotoxicity and protein kinase C inhibition of arylpyrrolylmaleimides，Archiv der Pharmazie，2008，341(5), 273-280 32. Xu GQ; Guo P; Zhang C; He QJ; Yang B; Hu YZ. Synthesis and Cytotoxicity of Indolopyrrolemaleimides，Chemical & Pharmaceutical Bulletin, 2007, 55(9), 1302-1307 授权发明专利： 1. 姜玉钦，李伟，赵杰，徐桂清等.一种表达COVID-19抗原的表达载体及基因工程乳酸菌口服疫苗的构建方法（ZL202010677960.7），授权日期：2023-09-08 2. 姜玉钦，丁清杰，马春华，徐桂清等. Substituted imidazolecarboxamide as Bruton's Tyrosine Kinase inhibitors（PCT/CN2020/133938），授权日期：2021-12-04 3. 姜玉钦，丁清杰，马春华，徐桂清等.Substituted 1-amino-1H-imidazole-5-carboxamide as Bruton's Tyrosine Kinase inhibitors（PCT/CN2020/089407），授权日期：2020-05-19 4. 訾明慧，徐桂清等.一种自动化性能高的化学反应检测装置（ZL201811343276.4），授权日期：2020-09-29 5. 柴荣荣，毛龙飞，徐桂清等.一种有机自动萃取装置（ZL201821860516.3），授权日期：2019-07-23 6. 徐桂清，高原等. 一种强力霉素的高效制备方法（ZL 2017102271420.5）. 授权日期：2019-05-31 7. 徐桂清，张银贵等. 一种强力霉素的制备方法（ZL 201710227183.4）. 授权日期：2019-05-17 8. 李伟，徐桂清等. 一种3,3,5,5-四甲基联苯胺的制备方法（ZL 201611014357.0）. 授权日期：2019-02-01 9. 徐桂清，姜玉钦等. 一种硫普罗宁及其锌配合物的制备方法（ZL 201610117530.X）. 授权日期：2018-07-13 10. 徐桂清，贾淑红等. 一种测定(4R, 6R)-6-胺乙基-2,2-二甲基-1,3-二氧六环-4-乙酸叔丁酯含量的方法（ ZL 201510497319.4）. 授权日期：2017-01-25 11. 徐桂清，孔端阳等. 具有抗菌活性的马来酰亚胺-1,2,3-三氮唑类化合物及其制备方法（ ZL 201310384113.1）. 授权日期：2014-08-20 12. 徐桂清，王晓锦等. 具有抑菌活性的烯唑醇-1,2,3-三氮唑类化合物及其制备方法（ZL 201310005915.7）. 授权日期：2015-05-06 13. 徐桂清，姜玉钦等. 具有抑菌活性的吲哚及其衍生物-三氮唑类化合物及其制备方法（ZL 201210328217.6）. 授权日期：2014-02-12 14. 姜玉钦，徐桂清等. 具有抗真菌活性的丹皮酚-1,2,3-三氮唑类化合物及其制备方法（ZL 201210326824.9）. 授权日期：2014-08-13 15. 姜玉钦，徐桂清等. 具有抑菌活性的苯并咪唑-1,2,3-三氮唑类化合物及其制备方法（ZL 201310005920.8）. 授权日期：2014-03-19技术转让、获奖及科技成果鉴定: 1. 技术转让：阿托他伐汀钙关键中间体及系列BTK抑制剂新药专利转让，2022.2，100万元。 2. 河南省科技成果鉴定：生物合成(R)－邻氯扁桃酸甲酸关键技术研究，豫科鉴委字〔2013〕第1530号，第二完成人。 3. 河南省科技成果鉴定：双膦酸盐骨吸收抑制剂新工艺研究及产业化，豫科鉴委字〔2009〕第524号。 4. 河南省科技成果鉴定：吉西他滨盐酸盐生产新工艺研究，豫科鉴委字(2009)第523号。 荣誉与奖励 1. 河南省科技创新杰出青年 2. 吉西他滨盐酸盐生产新工艺研究，河南省科技进步三等奖（第一完成人），2013 3. 曲克芦丁合成关键技术创新及产业化，河南省教育厅科技成果一等奖（第四完成人），2020 4. 多次获得河南师范大学优秀教师、“三育人”先进个人、优秀指导教师等 |