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Emergent synthetic methods for the modular advancement of sp3-rich fragments

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C–H functionalisation tolerant to polar groups could transform fragment-based drug discovery (FBDD)

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Pursuing high efficiency in photocatalytic oxidative couplings of heteroarenes and aliphatic C–H bonds

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Visible-light-mediated three-component Minisci reaction for heteroarylethyl alcohols synthesis

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Is it time for biocatalysis in fragment-based drug discovery?

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Visible-light- and bromide-mediated photoredox Minisci alkylation of N-heteroarenes with ester acetates

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Modular Synthetic Platform for the Elaboration of Fragments in Three Dimensions for Fragment-Based Drug Discovery

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Fragment-to-Lead Medicinal Chemistry Publications in 2019

Wolfgang Jahnke, Daniel A. Erlanson, Iwan J. P. de Esch, Christopher N. Johnson, Paul N. Mortenson, Yuji Ochi and Tatsuya Urushima

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High‐Throughput Optimization of Photochemical Reactions using Segmented‐Flow Nanoelectrospray‐Ionization Mass Spectrometry**

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Angew Chem Int Ed, 2023, 62
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High‐Throughput Optimization of Photochemical Reactions using Segmented‐Flow Nanoelectrospray‐Ionization Mass Spectrometry**

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Angewandte Chemie, 2023, 135
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Advanced Synthesis Using Photocatalysis Involved Dual Catalytic System

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Eur J Org Chem, 2022, 2022
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Switchable, Reagent‐Controlled Diastereodivergent Photocatalytic Carbocyclisation of Imine‐Derived α‐Amino Radicals

J. Andrew P. Maitland, Jamie A. Leitch, Ken Yamazaki, Kirsten E. Christensen, Doyle J. Cassar, Trevor A. Hamlin and Darren J. Dixon

Angewandte Chemie, 2021, 133, 24318
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Metallaphotoredox-Mediated Decarboxylative Cross-Coupling of α-Oxy Morpholine Carboxylic Acids and (Hetero)Aryl Halides

Jack L. Sloane, Anna Beatriz Santos, Eric M. Simmons and Trevor C. Sherwood

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Recent Advances in Minisci-type Reactions and Applications in Organic Synthesis

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COC, 2021, 25, 894
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Photoinduced α‐C−H Amination of Cyclic Amine Scaffolds Enabled by Polar‐Radical Relay

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Angew Chem Int Ed, 2022, 61
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Modular Synthesis of Heterobenzylic Amines via Carbonyl Azinylative Amination

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Targeting NRF2 to treat cancer

Jared Sivinski, Donna D. Zhang and Eli Chapman

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A Perspective on the Analytical Challenges Encountered in High-Throughput Experimentation

Rachel Grainger and Stuart Whibley

Org. Process Res. Dev., 2021, 25, 354
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Visible‐Light‐Induced Diastereoselective Cascade Cyclization to Construct Polycyclic Spiroindolines

Vadithya Ranga Rao, Vadla Shiva Prasad, Dharavath Ravi, Chelukalapally Anil Kumar, Sunil Kumar Nechipadappu and Praveen ReddyAdiyala

Adv Synth Catal, 2024, 366, 3303
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Photoredox Catalysis toward 2-Sulfenylindole Synthesis through a Radical Cascade Process

Marilia S. Santos, Hugo L. I. Betim, Camila M. Kisukuri, Jose Antonio Campos Delgado, Arlene G. Corrêa and Márcio W. Paixão

Org. Lett., 2020, 22, 4266
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Photocatalytic Late-Stage C–H Functionalization

Peter Bellotti, Huan-Ming Huang, Teresa Faber and Frank Glorius

Chem. Rev., 2023, 123, 4237
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Development of Photoredox Cross-Electrophile Coupling of Strained Heterocycles with Aryl Bromides Using High-Throughput Experimentation for Library Construction

Yukiko Mori, Mutsuyo Hayashi, Ryuma Sato, Kuninori Tai and Tsuyoshi Nagase

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Photocatalysis in the Life Science Industry

Lisa Candish, Karl D. Collins, Gemma C. Cook, James J. Douglas, Adrián Gómez-Suárez, Anais Jolit and Sebastian Keess

Chem. Rev., 2022, 122, 2907
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Diversification of Unprotected Alicyclic Amines by C−H Bond Functionalization: Decarboxylative Alkylation of Transient Imines

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Angew Chem Int Ed, 2021, 60, 1625
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Rupert S. J. Proctor and Robert J. Phipps

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Gram-Scale Domino Synthesis in Batch and Flow Mode of Azetidinium Salts

Alessandra Sivo, Vincenzo Ruta and Gianvito Vilé

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Photoinduced α‐C−H Amination of Cyclic Amine Scaffolds Enabled by Polar‐Radical Relay

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Angewandte Chemie, 2022, 134
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Expeditious and Automated Dispensing of ChemBeads for High-Throughput Experimentation in 384-Well Microtiter Plates

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Org. Process Res. Dev., 2025, 29, 2124
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High-Throughput Electrochemistry: State of the Art, Challenges, and Perspective

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Org. Process Res. Dev., 2021, 25, 2587
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Graphically Defined Model Reactions Are Extensible, Accurate, and Systematically Improvable

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Continuous Flow Photochemistry for the Preparation of Bioactive Molecules

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Molecules, 2020, 25, 356
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Parallel photoreactor development with enhanced photon efficiency and reproducibility based on laws of optics

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Fragments: where are we now?

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Rapid Optimization of Photoredox Reactions for Continuous-Flow Systems Using Microscale Batch Technology

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ACS Cent. Sci., 2021, 7, 1126
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Acridine/Lewis Acid Complexes as Powerful Photocatalysts: A Combined Experimental and Mechanistic Study

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ACS Catal., 2024, 14, 14574
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Jenseits von Friedel und Crafts: immanente Alkylierung von C‐H‐Bindungen in Arenen

Gwilherm Evano and Cédric Theunissen

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Modular Synthesis of Heterobenzylic Amines via Carbonyl Azinylative Amination

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Angew Chem Int Ed, 2024
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Synthesis of Soluble Quinacridone Photocatalysts for the Homogeneous Oxidation of Thioethers

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Eur J Org Chem, 2023, 26
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Developments and challenges in hit progression within fragment-based drug discovery

Harold Grosjean and Philip C. Biggin

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Photoredox-based late-stage functionalization in SAR study for in vivo potent glucosylceramide synthase inhibitor

Junsi Wang, Matthew Reynolds, Ignacio Ibáñez, Yusuke Sasaki, Yuta Tanaka, Fumiaki Kikuchi, Tomohiro Ohashi, Sho Sato, Mariko Miyabayashi, Takahiro Fujii and Yuta Tanaka

Bioorganic & Medicinal Chemistry Letters, 2022, 77, 129039
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Parallel and Flow Photoredox Chemistry Enabled by Advanced Temperature-Controlled Photoreactors

Oleg Borodin and Matthias Schmid

ACS Sustainable Chem. Eng., 2025, 13, 7750
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Surgical Cleavage of Unstrained C(sp3)−C(sp3) Bonds in General Alcohols for Heteroaryl C−H Alkylation and Acylation

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Merger of Single-Atom Catalysis and Photothermal Catalysis for Future Chemical Production

Junchuan Sun, Guanwu Lian, Zhongxin Chen, Zhigang Zou and Lu Wang

ACS Nano, 2024, 18, 34572
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Advancement in Organic Synthesis Through High Throughput Experimentation

Shruti A. Biyani, Yuta W. Moriuchi and David H. Thompson

Chemistry Methods, 2021, 1, 323
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Back in Person: Frontiers in Medicinal Chemistry 2023

Matthias Gehringer, Felix Pape, María Méndez, Philipp Barbie, Andrea Unzue Lopez, Julien Lefranc, Franca‐Maria Klingler, Gerhard Hessler, Thierry Langer, Eleonora Diamanti and Matthias Schiedel

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LiBr‐Promoted Photoredox Minisci‐Type Alkylations of Quinolines with Ethers

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Emerging concepts in photocatalytic organic synthesis

Susanne Reischauer and Bartholomäus Pieber

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Recent Advances in Visible-Light-Mediated Minisci Reactions

Jianyang Dong, Yuxiu Liu and Qingmin Wang

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Thiol-Mediated α-Amino Radical Formation via Visible-Light-Activated Ion-Pair Charge-Transfer Complexes

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Diversification of pharmaceutical molecules via late-stage C(sp2)–H functionalization

Weidong Shang, Hongbao Sun, Wei Chen and Jie Liu

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Automated Intelligent Platforms for High‐Throughput Chemical Synthesis

Jia-Min Lu, Jian-Zhang Pan, Yi-Ming Mo and Qun Fang

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Diversification of Unprotected Alicyclic Amines by C−H Bond Functionalization: Decarboxylative Alkylation of Transient Imines

Anirudra Paul, Jae Hyun Kim, Scott D. Daniel and Daniel Seidel

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Emerging trends in the optimization of organic synthesis through high-throughput tools and machine learning

Pablo Quijano Velasco, Kedar Hippalgaonkar and Balamurugan Ramalingam

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Synthesis of Chiral Amines by C–C Bond Formation with Photoredox Catalysis

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Process analytical technologies and self-optimization algorithms in automated pharmaceutical continuous manufacturing

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Visible-Light Photocatalysis as an Enabling Technology for Drug Discovery: A Paradigm Shift for Chemical Reactivity

Peijun Li, Jack A. Terrett and Jason R. Zbieg

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Technological Innovations in Photochemistry for Organic Synthesis: Flow Chemistry, High-Throughput Experimentation, Scale-up, and Photoelectrochemistry

Laura Buglioni, Fabian Raymenants, Aidan Slattery, Stefan D. A. Zondag and Timothy Noël

Chem. Rev., 2022, 122, 2752
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PIFA-mediated room temperature dehydrogenative annulation for the synthesis of 2-alkenyl oxazoles

Kang Chen, Jie-Ping Wan, Liyun Zhou and Yunyun Liu

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Beyond Friedel and Crafts: Innate Alkylation of C−H Bonds in Arenes

Gwilherm Evano and Cédric Theunissen

Angew Chem Int Ed, 2019, 58, 7558
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Accelerated Chemical Reaction Optimization Using Multi-Task Learning

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Synergy of Machine Learning and High‐Throughput Experimentation: A Road Toward Autonomous Synthesis

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New Strategies for the Transition-Metal Catalyzed Synthesis of Aliphatic Amines

Aaron Trowbridge, Scarlett M. Walton and Matthew J. Gaunt

Chem. Rev., 2020, 120, 2613
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α-Heteroarylation of Thioethers via Photoredox and Weak Brønsted Base Catalysis

Edwin Alfonzo and Sudhir M. Hande

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Regio‐ and Stereocontrolled‐Synthesis of a Heterocycle Fragment Collection Using Palladium Catalyzed C‐H Arylation

Amalia‐Sofia Piticari, Daniele Antermite, Harry J. Linkhorn, Natalia A. Larionova, Matthew P. Webster and James A. Bull

Chemistry A European J, 2025, 31
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Suzuki Miyaura cross-coupling of 2-chloropyrazine with arylboronic acids catalyzed by novel palladium(II) ONO pincer complexes

C. Shalini, N. Dharmaraj, Nattamai S.P. Bhuvanesh and M.V. Kaveri

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A Decarboxylative Cross-Coupling Platform To Access 2-Heteroaryl Azetidines: Building Blocks with Application in Medicinal Chemistry

James T. Brewster, Samuel D. Randall, John Kowalski, Cole Cruz, Richard Shoemaker, Eugene Tarlton and Ronald J. Hinklin

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A Brief Introduction to Chemical Reaction Optimization

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Shining a Light on the Advances, Challenges and Realisation of Utilising Photoredox Catalysis in Pharmaceutical Development

Emily E. Callard‐Langdon, Alan Steven and Rachel J. Kahan

ChemCatChem, 2023, 15
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Stereoselective Palladium‐Catalyzed C(sp3)−H Mono‐Arylation of Piperidines and Tetrahydropyrans with a C(4) Directing Group

Amalia‐Sofia Piticari, Daniele Antermite, Joe I. Higham, J. Harry Moore, Matthew P. Webster and James A. Bull

Adv Synth Catal, 2022, 364, 1488
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Deliberately Losing Control of C−H Activation Processes in the Design of Small‐Molecule‐Fragment Arrays Targeting Peroxisomal Metabolism

Raysa Khan Tareque, Storm Hassell‐Hart, Tobias Krojer, Anthony Bradley, Srikannathasan Velupillai, Romain Talon, Michael Fairhead, Iain J. Day, Kamlesh Bala, Robert Felix, Paul D. Kemmitt, Paul Brennan, Frank von Delft, Laura Díaz Sáez, Kilian Huber and John Spencer

ChemMedChem, 2020, 15, 2513
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α-C–H/N–H Annulation of Alicyclic Amines via Transient Imines: Preparation of Polycyclic Lactams

Weijie Chen and Daniel Seidel

Org. Lett., 2021, 23, 3729
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Neue Entwicklungen auf dem Gebiet der Minisci‐Reaktion

Rupert S. J. Proctor and Robert J. Phipps

Angewandte Chemie, 2019, 131, 13802
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Visible-Light-Mediated C–H Alkylation of Pyridine Derivatives

Fatima Rammal, Di Gao, Sondes Boujnah, Annie−Claude Gaumont, Aqeel A. Hussein and Sami Lakhdar

Org. Lett., 2020, 22, 7671
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α-C–H Bond Functionalization of Unprotected Alicyclic Amines: Lewis-Acid-Promoted Addition of Enolates to Transient Imines

Jae Hyun Kim, Anirudra Paul, Ion Ghiviriga and Daniel Seidel