基本信息
陈越磊  男  硕导  中国科学院上海药物研究所
电子邮件: chenyl@simm.ac.cn
通信地址: 上海市浦东新区祖冲之路555号5407室
邮政编码:

研究领域

药物化学,糖类药物化学,核苷药物化学。


招生信息

   
招生专业
100701-药物化学
招生方向
药物化学,糖类药物化学,核苷药物化学

教育背景

2004-10--2007-08   University of Muenster, 德国   博士学位
2001-09--2004-07   上海医药工业研究院   硕士学位
1997-09--2001-07   中国药科大学   学士学位

工作经历

   
工作简历
2010-07~现在, 中国科学院上海药物研究所, 副研究员
2009-02~2010-06,University of Minnesota, Twin Cities, 美国, 博士后
2007-10~2009-02,University of Muenster, 德国, 博士后

专利与奖励

   
奖励信息
(1) 2017年第二十届中国药学会-施维雅青年药物化学奖, , 部委级, 2017

出版信息

   
发表论文
(1) Stereoselective N-glycosylation with N4-acyl cytosines and efficient synthesis of gemcitabine, Tetrahedron, 2019, 通讯作者
(2) Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor, Bioorganic & Medicinal Chemistry Letters, 2019, 通讯作者
(3) Convenient preparation of pinometostat and related 5′-deoxy-5′-amino adenosine derivatives as well as their activity against DOT1L, Tetrahedron Letters, 2018, 通讯作者
(4) Efficient Syntheses of alpha- and beta-C-Nucleosides and the Origin of Anomeric Selectivity, Organic Chemistry Frontiers, 2018, 通讯作者
(5) Preparation of 5′-deoxy-5′-amino-5′-C-methyl adenosine derivatives and their activity against DOT1L, Bioorganic & Medicinal Chemistry Letters, 2017, 通讯作者
(6) Stereoselective addition of Grignard reagents to (2-methyl-5-tert-butyl)phenyl 1-thio-β-D-ribopentodialdo-1,4-furanoside derivative, Tetrahedron, 2017, 通讯作者
(7) A One-pot Synthesis of Omarigliptin and Its Analogues via Stabilized beta-Amino Ketone Intermediate., Synthetic Communications, 2017, 通讯作者
(8) Stereoselective and Regioselective Preparations of C-Pentopyranosides and Formal Synthesis of Omarigliptin., European Journal of Organic Chemistry, 2016, 通讯作者
(9) Formation of 1,3-diazocine by palladium catalyzed C–H arylation, Tetrahedron Lett., 2016, 通讯作者
(10) Multi-substituted 8-aminoimidazo[1,2-a]pyrazines by Groebke-Blackburn-Bienayme reaction and their Hsp90 inhibitory activity, Organic & Biomolecular Chemistry, 2015, 通讯作者
(11) Condensed Fukui function predicts innate C-H radical functionalization sites on multi-nitrogen containing fused arenes, RSC Advances, 2014, 通讯作者
(12) A Novel Strategy for Preparing Glycopeptide Molecular Probe Using Fluorous Technology, Protein Pept. Lett., 2014, 通讯作者
(13) Neoglycopeptide Synthesis by Suzuki-Miyaura Couplings between Glycosyl Aryl Boronic Acids and Iodopeptides, Protein Pept. Lett., 2014, 通讯作者
(14) 1,2-trans-1-Dihydroxyboryl benzyl S-glycoside as glycosyl donor, Carbohydrate Research, 2014, 通讯作者
(15) Highly Stereoselective Nucleophilic Addition of Difluoromethyl-2-pyridyl Sulfone to Sugar Lactones and Efficient Synthesis of Fluorinated 2-Ketoses, European Journal of Organic Chemistry, 2014, 通讯作者
(16) Direct Glycosylation of Bioactive Small Molecules with Glycosyl Iodide and Strained Olefin as Acid Scavenger, The Journal of Organic Chemistry, 2014, 通讯作者
(17) Strained olefin enables triflic anhydride mediated direct dehydrative glycosylation, Organic & Biomolecular Chemistry, 2014, 通讯作者
(18) (N,N-Diisopropylcarbamoyloxy)-methyl p-tolyl sulfone: preparation and application for the syntheses of 1,2-diols, Tetrahedron, 2012, 通讯作者
(19) C-6 aryl substituted 4-quinolone-3-carboxylic acids as inhibitors of hepatitis C virus, Bioorganic & Medicinal Chemistry, 2012, 第 1 作者
(20) The design, synthesis and biological evaluations of C-6 or C-7 substituted 2-hydroxyisoquinoline-1,3-diones as inhibitors of hepatitis C virus, Bioorganic & Medicinal Chemistry, 2012, 第 1 作者
(21) Copper-catalyzed asymmetric addition of Et2Zn to 2-cyclohexen-1-one and 2-carbamoyloxy-2-cyclohexen-1-one with phosphoramidite, phosphite, and bidentate phosphite-oxazoline ligands, Tetrahedron-Asymmetry, 2009, 通讯作者
(22) Copper-catalyzed asymmetric conjugate addition of Grignard reagents to 1-(N,N-diisopropylcarbamoyloxy)-1-tosyl-1-alkenes, Tetrahedron-Asymmetry, 2009, 通讯作者
(23) 1-(N,N-Diisopropylcarbamoyloxy)-1-tosyl-1-alkenes-a(2)d(1) Synthons via Tandem Umpolung, The Journal of Organic Chemistry, 2009, 通讯作者
(24) Protecting group manipulation on D-glucosamine propane-1,3-diyl dithioacetal, Journal of Carbohydrate Chemistry, 2007, 第 1 作者
(25) Preparation of 2-deoxystreptamine derivatives with all-axial substituents for desymmetrization, Tetrahedron Letters, 2007, 第 1 作者
(26) D-Glucosamine trimethylene dithioacetal derivatives: formation of six- and seven-membered ring amino carbasugars. Synthesis of (-)-calystegine B-3, Organic & Biomolecular Chemistry, 2007, 第 1 作者
(27) Propane-1,3-diyl dithioacetals of carbohydrates; Part 7: Preparation of aminocyclitols and iminosugars by intramolecular cyclizations of D-glucosamine propane-1,3-diyl dithioacetal derivatives, Synthesis, 2006, 第 1 作者
(28) Trimethylene dithioacetals of carbohydrates, part 6: C-C coupling reactions of dilithiated N-acetyl-D-glucosamine trimethylene dithioacetal derivatives, Synthesis, 2006, 第 1 作者
(29) 拉米夫定合成路线图解, 中国医药工业杂志, 2005, 第 1 作者
(30) 卡培他滨类似物的合成及体内抗肿瘤活性, 中国药物化学杂志, 2004, 第 1 作者
(31) Recent advances in conversion from carbohydrates to functionalized carbocycles, Chinese Journal of Organic Chemistry, 2004, 通讯作者
(32) A facile one-pot synthesis of N-4-alkyloxycarbonyl cytosine nucleosides, Synthetic Communications, 2004, 通讯作者

科研活动

   
科研项目
( 1 ) 靶向 DOT1L的抗血液肿瘤个性化先导化合物发现研究, 主持, 部委级, 2016-01--2017-12
( 2 ) 表观遗传重要靶点 MLL1 的候选药物发现, 主持, 国家级, 2014-01--2016-12
( 3 ) 用于制备核苷类药物的糖苷化反应研究, 参与, 市地级, 2015-09--2017-08
( 4 ) Omarigliptin 实验室合成工艺研究, 主持, 院级, 2014-01--2017-12
( 5 ) 新型DOT1L抑制剂的构效构代关系研究, 主持, 国家级, 2017-01--2018-12
( 6 ) TCP 衍生LSD1 抑制剂的脱靶作用研究和先导化合物优化, 主持, 国家级, 2019-01--2022-12
( 7 ) Omarigliptin 原料药制备工艺及质量标准研究, 主持, 院级, 2014-01--2034-12
( 8 ) 基于结构的蛋白激酶TNIK 靶向个性化药物设计, 主持, 部委级, 2019-01--2020-12
( 9 ) MEK1/2-HDAC 双重抑制剂的研究, 主持, 国家级, 2011-01--2014-12