|
-
个人简介
药学院、绿色制药协同创新中心机械化学研究所骨干教师,机械化学研究所师生联合党支部书记,浙江省化学会机械化学专业委员会副主任委员,浙江省药学会药物化学与抗生素专业委员会青年分委会委员,浙江省可持续发展研究会会员。
2024年入选浙江省高层次人才特殊支持计划-科技青年人才,2015年入选浙江省151人才工程第三层次培养计划,2016年入选浙江省青年科学家培养计划。主要研究方向为机械化学制药,可持续药物分子构建方法开发。聚焦医药化学品生产过程中的反应转化控制与可持续性发展的核心问题,构建基于机械化学的绿色合成新方法。实现抗虫药左旋吡喹酮、抗肿瘤药阿西替尼、抗疟药物乙胺嘧啶,肌肉松弛剂丹曲洛林,抗哮喘药物孟鲁司特钠,杀菌剂啶酰菌胺,吲哚天然产物(Streptindole、Nomofungin/Communesin B),Nigellidin类似物,PLK4抑制剂,类固醇激素核受体调节剂等多种药物及天然产物的绿色合成。
主持国家自然科学基金项目3项、浙江省自然科学基金项目2项,其他省部级及企业合作项目5项。作为主要成员参与国家重点研发计划项目、973计划前期研究专项等国家级项目5项。Nature Catalysis., Chem Catal., Nature Commun., Green Chem.等10余期刊审稿人,在国际高影响力期刊上发表SCI论文45篇(H-index = 22),获授权发明专利13项,参与编写英文专著1部。
-
科研项目
n 国家自然科学基金面上项目,机械化学-光协同促进脂肪烃参与的不对称自由基接力偶联及机理研究,2025/01-2028/12,在研,主持;
n 浙江省基础公益研究计划项目,机械力作用下脂肪烯烃选择性偶联反应调控策略研究,2023/01-2025/12,在研,主持;
n 国家自然科学基金面上项目,基于机械化学的Fe催化(不对称)C-H键活化/C-C键偶联反应研究,2020/01-2023/12,结题,主持;
n 浙江省基础公益研究计划项目,左旋吡喹酮绿色合成工艺开发,2018/01-2020/12,结题,主持;
n 国家自然科学青年基金项目,无溶剂球磨条件下负载催化体系促进的不对称交叉脱氢偶联反应研究,2015/01-2017/12,结题,主持;
n 国家973计划前期研究专项课题,基于机械化学理论的不活泼卤代芳烃偶联及脱卤反应机制与应用基础研究,2014/09-2016/06,结题,参与;
n 国家重点研发计划项目,原料药工业菌种改造关键技术及产业示范,2021/07-2025/06,结题,参与。
n 企业委托项目,藏花酸及其凝胶乳制备工艺开发,2022/04-2023/03,结题,主持;
n 企业委托项目,药物核磁结构解析,2020/10-2022/12,结题,主持;
n 企业委托项目,光电化学品及其杂质的结构研究,2024/01-2026/05,在研,主持;
n 企业委托项目,腐蚀性物料分解动力学研究,2024/11-2025/05,结题,主持;
-
科研成果
1.论文专著
Yu, J. B.*; Chen, H.; Zhang, Z.-W.; Fang, Y.-X.; Ying, T.; Su, W.-K. Ethanol-assisted mechanochemical asymmetric cross-dehydrogenative coupling reaction with recoverable chiral amine/NaCl for accessing chiral α-alkyl α-glycine derivatives, Green Chem. 2024, 26, 6570–6577.
Yang, Y.-C.; Huang, Q.-N.; Miao, L.-P.; Zhang, Q.-H.; Wu, C.-Y. *; Su, W.-K., Yu, J.-B.* Chitosan/γ-polyglutamic acid-based pickering emulsion gel: A promising transdermal carrier for crocetin, Int. J. Biol. Macromol. 2025, 311, 144161.
Xiang, K.-Y.; Shou, H. W.; Hu, C.-H.; Su, W.-K.; Yu, J. B.* Mechanochemical aerobic oxidative Heck coupling by polymer-assisted grinding: cyclodextrin additive facilitating regioselectivity control, Green Chem. 2024, 26, 5890–5899.
Fan, H.-Q.; Fang, Y.-X. ; Yu, J.-B.* Direct alkene functionalization via photocatalytic hydrogen atom transfer from C(sp3)–H compounds: a route to pharmaceutically important molecules, Chem. Commun.2024, 60, 13796–13818.
Wu, C.-Y.; Lv, J.; Fan, H.-Q.; Su, W.-K.; Cai, X.-J.; Yu, J.-B.* Mechanochemical C–H arylation and alkylation of indoles using 3d transition metal and zero-valent magnesium, Chem. Eur. J. 2024, e202304231. (Hot paper)
Yu, J.-B.*; Zhang, Y.-H.; Zheng, Z.-H.; Su, W.-K.* Total mechano-synthesis of 2-cyclopropyl-4-(4-fluorophenyl)quinoline-3-acrylaldehyde—a pivotal intermediate of pitavastatin, RSC Mechanochem., 2024, 1, 367–374.
Hu, C.-H.; Xiang, K.-Y.; Ying, T.; Yu, J.-B.* Oxidative alkenylation of (hetero)aromatics with unactivated alkenes: control of the reaction selectivity,Adv. Synth. Catal. 2024, 366, 1922–1949. (Very Important Publication)
Ying, P.; Ying, T.; Chen, H. Xiang, K.-Y.; Su, W.-K.; Xie, H.-J.; Yu, J.-B.* , Iron-catalyzed asymmetric Csp3–H/Csp3–H coupling: improving the chirality induction by mechanochemical liquid-assisted grinding, Org. Chem. Front., 2024, 11, 127-134.
Xiang, K.-Y.; Ying, P.; Ying, T.; Su, W.-K.; Yu, J.-B.* α-C–H functionalization of glycine derivatives under mechanochemical accelerated aging en route the synthesis of 1,4-dihydropyridines and α-substituted glycine esters, Green Chem., 2023, 25, 2853-2862.
Wu, C.-Y.; Ying, T.; Fan, H.-Q.; Hu, C.-H.; Su, W.-K.; Yu, J.-B.*C‑4 Regioselective Alkylation of Pyridines Driven by Mechanochemically Activated Magnesium Metal, Org. Lett., 2023, 25, 2531–2536.
Yang, X.-J.; Wang, H.; Zhang, Y.-H.; Su, W.-K.; Yu, J.-B.* Generation of Aryl Radicals from in situ Activated Homolytic Scission: Driving Radical Reactions by Ball Milling, Green Chem., 2022, 24, 4557–4565.
Yang, X.-J.; Wu, C.-Y.; Su, W.-K.; Yu, J.-B.* Mechanochemical C-X/C-H Functionalization: An Alternative Strategic Access to Pharmaceuticals, Eur. J. Org. Chem. 2022, e202101440. (cover feature)
Wu, C.-Y.; Ying, T.; Yang, X.-J.; Su, W.-K.; Dushkin, A. V.; Yu, J.-B.* Mechanochemical Magnesium-Mediated Minisci C–H Alkylation of Pyrimidines with Alkyl Bromides and Chlorides, Org. Lett., 2021, 23, 16, 6423–6428.
Ying, P.; Yu, J.-B.*; Su, W.-K.* Liquid-Assisted Grinding Mechanochemistry in the Synthesis of Pharmaceuticals, Adv. Synth. Catal., 2021, 5, 1246–1271. (Hot paper, Highly cited paper, Wiley Top Cited Article 2021-2022)
Shou, H.-W.; He, Z.-T.; Peng, G.; Su, W.-K.; Yu, J.-B.* Two Approaches for the Aynthesis of Levo-Praziquantel, Org. Biomol. Chem., 2021, 19, 4507–4514.
Yu, J.-B.; Ying, P.; Wang, H.; Xiang, K.-Y.; Su, W.-K.* Mechanochemical Asymmetric Cross-Dehydrogenative Coupling Reaction: Liquid-Assisted Grinding Enables Reaction Acceleration and Enantioselectivity Control, Adv. Synth. Catal., 2020, 362, 893–902.
Yu, J.-B.; Yang, X.-J.; Wu, C.-Y.; Su, W.-K.* Palladium-Catalyzed C−H/C−H Cross Coupling by Mechanochemistry: Direct Alkenylation and Heteroarylation of N1-Protected 1H-Indazoles, J. Org. Chem., 2020, 85(2), 1009–1021.
Yu, J.-B.; Jiang, Z. J.; Su, W.-K., Ball Milling Towards Green Synthesis: Applications, Projects, Challenges (chapter 5), The Royal Society of Chemistry, 2015.
2.授权专利
一种藏红花酸的无溶剂制备方法,2024-3-26,中国,ZL202211036288.9
一种联杂芳烃类化合物及其制备方法,2022-4-26,中国,202110406890.6
一种7-烷基吲哚衍生物的制备方法, 2021-10-12, 中国, ZL201811504030.0
一种不活泼烯烃芳基化合物的制备方法, 2021-07-27, 中国, ZL201811504030.0
一种(R)-吡喹酮的制备方法, 2021-07-30, 中国, ZL202010099185.1
一种从丝状真菌中提取壳寡糖的方法, 2021-02-02, 中国, ZL201711493945.1.
一种(R)-吡喹酮中间体及(R)-吡喹酮的制备方法, 2019-09-10, 中国, ZL201810355575.3.
一种2,3-二取代吲哚衍生物的制备方法, 2018-05-08, 中国, ZL201610368881.1.
3-烯基吲哚类化合物的制备方法, 2017-09-29, 中国, ZL201510330391.8.
