药物合成反映是化学制药领域的主要环节!!!B躺悄拷窕Щち煊虻难芯咳让藕颓把!!!O衷谟谢铣晒赜诳蒲忠涨敖涂蛊鸬狡鹁⒌耐菩卸,深刻地改变着社会生产和生涯!!!4勇躺Ы嵌妊芯坑谢铣捎τ,探索绿色化学在有机合成中的应用情形,为化学合成工业提供绿色开展的可持续理念!!!
光化学反映平台
- 近年来可见光催化反映已经成为有机化学中的前沿领域,作为一种强盛的活化小分子的手段而起着不可替换的作用!!!9饣б炀哂蟹乔秩胄、反映速率快、时空可控等优点,普遍用于质料制备和改性的各个方面!!!=柚诠饣Х从车目煽赜肟墒拥亩劳逃攀,可从源头出发,建设生命科学研究的新手段、新要领、新手艺等!!!V还茉圃,仍然需要一直拓展和发明新的光活化模式来提高反映效率,扩大应用规模!!!

豪门国际官网光化学反映平台:
包括差别功率紫外光反映器(254/360nm),30W-1000W;;;蓝光反映器笼罩360-520nm波长规模;;;光催化剂:网络有常见金属催化剂和有机催化剂,并凭证文献一直扩充;;;毫摩级别流体反映器定制中C(sp3)-C(sp2) coupling reactions
Decarboxylative coupling
Proposed mechanistic pathway of nickel-catalyzed photoredox- decarboxylative arylation[1]C-H cross-coupling
Photoredox, HAT, and nickel-catalyzed cross-coupling: proposed mechanistic pathway and catalyst combination[2]C(sp3)-C(sp3) coupling reactions
Decarboxylative coupling
Carboxylic acid and alkyl halide scope in the dual nickel-catalyzed photoredox sp3-sp3 coupling reaction[3]C-H cross-coupling
The scope of the alkyl bromide coupling partner in the light-enabled selective sp3 C-H alkylation[4]Heteroatom arylations
C-N coupling
Metallaphotoredox-catalyzed amination: amine and arene scope[5]C-O coupling
Alcohol and aryl halide scope in the nickel-catalyzed photoredox C-O coupling reaction[6]Other reactions
Ar-X trifluomethylation
Synthesis of trifluoromethyl(hetero)arenes[7]Decarboxylative fluorination
Decarboxylative Fluorination of Aliphatic Carboxylic Acids via Photoredox Catalysis[8]
催化剂筛选平台
- 金属催化剂由于其特殊的催化活性,底物选择性而普遍应用在合成有机化学中!!!S绕浣鹗舸呋闹种峙剂从,可以快捷高效的形成种种碳碳键和碳杂原子键,因而在药物化学的研究中施展着极为要害的作用,也是有机化学很是主要的研究偏向!!!>萃臣,杂原子的烷基化/芳基化和碳碳键的形成反映是使用率最高的有机反映前五位之一!!!H欢,由于底物的多样重大性,金属催化偶联反映的失败率很高,如碳氮偶联的反映失败率在50%以上,由于许多药物分子中的杂环通常是催化剂抑制剂!!!2⑶以谝┪锓⒚鹘锥,由于项目研发时间紧迫,通常药物化学家手头可以探索反映的中心体数目有限!!!催化剂筛选可以完善的解决这个问题!!!Mü煽康拇呋疗叫猩秆,我们可以用数十毫克甚至更少量的中心体,在48小时甚至更短时间内获得差别的催化剂,配体,碱,溶剂和温度下的反映效果!!!???梢跃】熳龀黾绦钟絮杈短剿,或者放弃该蹊径合成的决议,而不会铺张太多时间,最后却以失败而了却!!!
催化剂筛选流程图

催化剂筛选示意图


催化剂筛选反映类型
Suzuki, Buchwald (C-N/O) 催化剂初筛系统已准备完毕催化剂筛选仪器装置

电化学反映平台
- 开展绿色可再生能源是未来开展的偏向,现在在生物质催化转化领域主要使用的照旧通俗的催化转化要领,许多反映需要在高温高压下举行,并且许多催化剂和溶剂都有毒性,会对情形带来污染!!!K孀啪蒙缁岬囊恢笨,绿色化学的要领在化学合成中的应用获得了越来越多的关注!!!S谢绾铣杀灰晕且恢智樾斡押玫、切合绿色化学要求的有机合成要领!!!5缁б煲蚓哂幸子谖⑿突、高迅速度、适合非透明样品、电源功率要求低等突出优势,特殊适合构建微型化剖析装置!!!
电化学定制示意图
Basic Components of an Undivided Electrochemical Cell[9]Synthetic organic electrochemistry applications
Ni-Catalyzed C-N coupling
Nickel-catalyzed amination of aryl halides[10]Ni catalyzed Sp2-Sp3 coupling
Reaction Scope for Electrochemical Cross-Electrophile Couplings[11]C-H Oxidations
Substrate scope of the electrochemical benzylic C–H oxidation reaction[12]Reduction of amide
Plausible reaction mechanism using a Zn anode[13]Heterocycles formation
Formation and cyclization of nitrogen-centered radicals[14]-OCF3, -SCF3, -CF3
Electrochemical Trifluoromethoxylation of (Hetero)aromatics[15]Fluorination
Electrochemical Fluorination of 2,2-Diphenyl-1,3-dithiolane[16]
总结- 绿色化学将是有机合成的主旋律!!!作为绿色化学的提倡者,豪门国际官网绿色化学平台由公司资深科研专家向导,驻足于绿色化学手艺, 将电化学、光化学、金属催化、酶催化及连续化生产等前沿绿色手艺整合到种种化学活性分子及中心体的化学合成蹊径中,对医药和化工行业现有小分子化药合成蹊径举行优化刷新,赋能豪门国际官网化学家和客户,提升研发项目的效率,镌汰化学合成方法,提高总体合效果率,降低情形污染,实现情形优化型的可持续合成反映!!!
参考文献- [1] Zhiwei Zuo,et al. Dual catalysis. Merging photoredox with nickel catalysis: coupling of α-carboxyl sp?-carbons with aryl halides. Science. 2014 Jul 25;345(6195):437-40. doi: 10.1126/science.1255525.[2] Megan H Shaw,et al. Native functionality in triple catalytic cross-coupling: sp? C-H bonds as latent nucleophiles. Science. 2016 Jun 10;352(6291):1304-8. doi: 10.1126/science.aaf6635.[3] Craig P Johnston, et al. Metallaphotoredox-catalysed sp(3)-sp(3) cross-coupling of carboxylic acids with alkyl halides. Nature. 2016 Aug 18;536(7616):322-5. doi: 10.1038/nature19056.[4] Chip Le,et al. Selective sp? C-H alkylation via polarity-match-based cross-coupling. Nature. 2017 Jul 6;547(7661):79-83. doi: 10.1038/nature22813.[5] Emily B Corcoran, et al. Aryl amination using ligand-free Ni(II) salts and photoredox catalysis. Science. 2016 Jul 15;353(6296):279-83. doi: 10.1126/science.aag0209.[6] Jack A Terrett, et al. Switching on elusive organometallic mechanisms with photoredox catalysis. Nature. 2015 Aug 20;524(7565):330-4. doi: 10.1038/nature14875.[7] Chip Le, et al. A radical approach to the copper oxidative addition problem: Trifluoromethylation of bromoarenes. Science. 2018 Jun 1;360(6392):1010-1014. doi: 10.1126/science.aat4133.[8] Sandrine Ventre, et al. Decarboxylative Fluorination of Aliphatic Carboxylic Acids via Photoredox Catalysis. J Am Chem Soc. 2015 May 6;137(17):5654-7. doi: 10.1021/jacs.5b02244.[9]Cian Kingston, et al. A Survival Guide for the "Electro-curious". Acc Chem Res. 2020 Jan 21;53(1):72-83. doi: 10.1021/acs.accounts.9b00539.[10] Chao Li, et al. Electrochemically Enabled, Nickel-Catalyzed Amination. Angew Chem Int Ed Engl. 2017 Oct 9;56(42):13088-13093. doi: 10.1002/anie.201707906.[11] Robert J Perkins, et al. Electrochemical Nickel Catalysis for sp2-sp3 Cross-Electrophile Coupling Reactions of Unactivated Alkyl Halides. doi: 10.1021/acs.orglett.7b01598. Org Lett. 2017 Jul 21;19(14):3755-3758.[12]Jason A Marko, et al. Electrochemical benzylic oxidation of C-H bonds. Chem Commun (Camb). 2019 Jan 17;55(7):937-940. doi: 10.1039/c8cc08768g.[13] Kazuhiro Okamoto, et al. Hydrosilane-Mediated Electrochemical Reduction of Amides. J Org Chem. 2021 Nov 19;86(22):15992-16000. doi: 10.1021/acs.joc.1c00931.[14] Huai-Bo Zhao, et al. Amidinyl Radical Formation through Anodic N-H Bond Cleavage and Its Application in Aromatic C-H Bond Functionalization. Angew Chem Int Ed Engl. 2017 Jan 9;56(2):587-590. doi: 10.1002/anie.201610715.[15] Yao Ouyang, et al. Electrochemical Trifluoromethoxylation of (Hetero)aromatics with a Trifluoromethyl Source and Oxygen. Angew Chem Int Ed Engl. 2022 Jan 17;61(3):e202114048. doi: 10.1002/anie.202114048.[16] Naoki Shida, et al. Alkali Metal Fluorides in Fluorinated Alcohols: Fundamental Properties and Applications to Electrochemical Fluorination. J Org Chem. 2021 Nov 19;86(22):16128-16133. doi: 10.1021/acs.joc.1c00692.










