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Integrated Discovery in action: from Fragment Library to promising pan-coronavirus pre-clinical candidate
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Advanced Oxetane Scaffolds: Synthesis, Stability, and Physicochemical Fine-Tuning for Medicinal Chemistry
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Advanced studies on the stability of the oxetane moiety in common organic synthesis transformations
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2,2-Difluorocyclopropanamine: Tentative Structure or Useful Building Block?
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Practical multigram synthesis and derivatization of Cuneane: Expanding access to a promising
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Chasing an elusive 1,5-oxazocane motif: A simple multigram approach to a rare chemotype
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"Fingerprint": a method for quick quality control of catalysts for heterogeneous hydrogenation
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Flow (hetero)aromatic Li-organic generation via H/Li and Br/Li exchange: scope and limitations
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Spirocyclic β-prolines with a δ-spiro fusion: Expanding the 3D chemical space for MedChem purposes
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gem-Difluorinated saturated O- and N-heterocycles - the new tools for fine tuning of physicochemical properties
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Organozinc Compounds in N,N-Dimethylformamide: Stability Towards Degradation And Reactivity in Negishi Cross-Coupling Reactions
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In-flow Generation of Diverse Zn-organics for the MedChem Libraries via Parallel Synthesis
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Generating Library Comprehensive 3-D-Shape Building Blocks of Spirocyclic a- and b-prolines
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Deoxyfluorinative approach towards fluorine-substituted organoboronates
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One-step Scalable Access to Benzo-Fused Imidazoles and Oxazoles: A Cost-Effective and EcoFriendly Approach
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Petasis / Grubbs Reactions Sequence as an example of using DOS-like strategy to the MedChem relevant building blocks synthesis
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Synthesis and Functionalization of Azabicyclo[2.2.1] heptanes for Medicinal Chemistry Applications
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Intramolecular "substituent transferring" from alkynes to furans: scope and limitations
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γ-Functionalized α-CF
3
-substituted derivatives of tetrahydrofuran and tetrahydrothiophene: synthesis and physicochemical evalution
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Selective Pd-Catalyzed Carbonylation of Polyhalogenated (Hetero)Arenes: A Role of Temperature and Electronic Effects of Substituents
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Versatile Synthetic Pathways to Heteroadamantane Cages; Enhancing Accessibility and Functionality
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An Unprecedented Pathway to Fused Imidazole Derivatives from Azine Carboxamides: Scope, Limitations, and Mechanistic Insights
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SF
4
as a deoxofluorinating reagent. Is it green or hazardous?
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Chasing Elusive Chemotypes: A Unified Strategy Toward Functionalized 7- and 8-Membered Oxaza-Heterocycles
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In-flow organolithium/magnesium/zinc compounds vs batch classical approaches
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3,3-Disubstituted Oxetanes for Medicinal Chemistry Needs: The Technical Guide
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Neglected Cage Compounds from Rare Structures to Available Chemicals
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Rhenium heptasulfide: rebirth as selective hydrogenation catalyst for organic synthesis
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@nmr_spectroscopy: A Social Media-Based Educational Project Focused on Small Molecule NMR
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Integrated platform for rapid PROTACs discovery: Case Study Targeting BRD4
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Assessing PROTAC Permiability and Protein Bilding: Challenged and Assay Optimization
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REAL approach to developing CRBN molecular glue libraries and E3 ligand-linker conjugate kits
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Integrated Drug Discovery from Hit Generation to Preclinical Candidate with Enamine Discovery Switzerland
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Integrated PROTAC Discovery Platform: From Design To BRD4 Degradation
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Versatile Synthesis of Drug-like Methyl Sulfones and Analogues for Medicinal Chemistry
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3-oxabicyclo[3.1.1]heptanes as sp
3
-Rich Meta-Benzene Isosteres for Drug Design
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Photochemical Access to Drug-like Alkyl Azetidines: Batch and Flow Strategies
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Biotransformation of bicyclic amides by
Cunninghamella elegans
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Practical Multigram Synthesis of Functionalized Homomorpholines and Their Further Application
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Synthetic Toolbox to Diverse Sets of α-Prolines with Spiro-Linkage
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Trimethylsilyltrifluoromethane – Effective Difluorocarbene-Surrogate for Scalable Organic Synthesis
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Single-Step Semi-Industrial Synthesis of 2-Alkyl-Substituted Benzo- and Hetoroannelated 1,3-Azoles
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New Covalent Probes: parallel synthesis of covalent binders and their application in early discovery
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Diels-Alder guided domino avenue to a Medchem relevant condensed furan platform
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Safe, flow generation of "Dry diazomethane" in multigram scale for preparation Medchem relevant building blocks
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Fine physico-chemical tuning using "small" structural variation: Fluorine case
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Fluorinated Oxetanes: Fine-tuning of Physicochemical Properties of 3,3-disubstituted Building Blocks
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New synthetic instruments to reach 2,2-spiro-beta-proline molecular platform
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Up-Scale Diazomethane Generation in Flow: Safe Handling and Broad Use in Organic Synthesis
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A Leap Toward Incorporating Oxetane Core into MedChem Relevant Compounds
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Light-enabled Scalable Synthesis of Bicyclo[1.1.1]pentane halides and their functionalizations
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Creating cocktails for
19
F NMR-assisted FBDD approach based on Enamine’s in-stock collection
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Neglected Cage Compounds – Transitioning From Rare Molecules to Casual MedChem Tools
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Cell painting technique for phenotypic profiling of newly synthesised piperine analogues
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Identifying novel covalent allosteric inhibitors of WEE1 protein kinase
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Divergent Approach to Diazoketones Photochemistry
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CF
2
OMe-decorated aliphatic amines as perspectives building blocks for medicinal chemistry
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Efficient access to (het)arylacetic acids: one step for synthetic chemistry, a leap for drug design research
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Comprehensive oxetane building block’s library: through a prism of 10 years’ experience
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Diversity-oriented access to conformationally restricted δ-amino acids – a tool for the design of peptide-like foldamers
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Sonidegib bioisosteres: activity and ADME properties
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2-Oxabicyclo[2.1.1]hexane as saturated bioisostere of Fluxapyroxad: synthesis and antifungal activity
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Spiro[3.3]heptane as a Benzene Bioisostere for Drug Discover
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The activity of Benzocaine benzene ring bioisosteres
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Optimization of the Assay Conditions to Increase Recovery in Caco-2 Permeability Assay for PROTACs
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Functionalized bicyclic tetrahydrofurans: practical approach to CCR2 antagonist precursors
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DOS-like strategy for the Medchem relevant building blocks via Petasis/Grabbs reaction
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Synthesis of 6-azaindoles with “unusual” substitution pattern
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Safe, Multigram Flow Generation of Diazomethane for Organic Synthesis
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Advanced Medchem relevant library of functionalized oxetanes
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Medchem Perspectives of Bis-Nor-Adamantane (Stellane) & Nor-Adamantane Derivatives
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Practical avenues to a complete set of spiro-linked alpha-prolines
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2-Substituted [1,2]-cycloannelated pyrrolidines and piperidines in the focus of medicinal chemistry
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Borylated cyclobutanes via thermal [2+2]-cycloaddition
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Spiro[3.3]heptane as a Saturated Benzene Bioisostere
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2-Oxabicyclo[2.2.2]octane bioisostere of Vorinostat: synthesis and biological activity
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Establishing the lschemia-Reperfusion Model in Rats for Chronic Renal Pathology Investigations
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Sonidegib bioisosteres: activity and ADME properties
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An "Ideal" Bioisoster of the
para
-substituted Phenyl Ring
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Assessing the Efficacy of Various Kidney Injury Parameters in Predicting Acute Kidney Injury Outcomes
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Novel Class of Piperidine Bioisosteres
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The activity of Benzocaine benzene ring bioisosteres
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3-CF
3
/C
2
F
5
- Substituted Proline Analogs: Synthesis and Proteolytic Stability of Their Amide Derivatives
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Chemical Landscape of Capping Agents for DNA-Encoded Technologies (DELT) from Enamine Perspective
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Diagonally protected 1-methylcyclobutane 1,3-diamines in Abrocitinib analogues synthesis
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Easy-to-perform large scale approach to 1-methyladamantane and its derivatives – scarce though prominent medchem building-blocks
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Efficient one-step approach to annulated tetrahydrofurans: supporting the search for new potent CCR2 receptor antagonists
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Thermal [2+2] synthesis of 3-oxocyclobutyl boronates
via
keteniminium salts
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Unexpected isomerization of azetidine-carboxylic acids
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Electrophilic [4+1]-cyclization of picolines – efficient avenue towards 6-azaindole and 6-azabenzofuranes
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gem
-Difluoromethylene Decorated cyclic building blocks - impact on physicochemical properties
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Looking for an ideal HTS screening collection
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Novel chemotypes of angiotensin-converting enzyme 2 binders
via
successive
in silico
screening and
in vitro
evaluation approaches
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Polyfunctional Core Building Blocks for DNA-Encoded Technologies (DELT): the Definitive Factor for Libraries Diversity
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Synthesis of annulated azinopyrol heterocyclic frameworks as purine analogs
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Synthesis of versatile stellane derivatives in multigram scale
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Design and synthesis of purines analogs based on different annelated azines
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COD – the promising source for diverse cage-divergent cores
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Semi-industrial synthesis of 2-alkyl-substituted benzothiazoles
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The impact of substituents and cycle size on the regioselectivity of Beckman rearrangement in annelated cyclic ketones
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Intramolecular Diels-Alder reaction of alkynyl substituted furanes as an efficient way to rare furan-contained MedChem relevant building blocks
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The assembly of fused pyridazines
via
one-pot sequence IEDDA reaction, scope and limitations
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Practical access to conformationally restricted β-prolines with 2,2-spiro-conjugation
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Regioselectivity study of Beckman reaction as a pathway for synthesis of bicyclic anilines and benzylamines
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Robust multigram protocol to access diazaspiroalkanes featuring azetidine moiety
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Easy access to enantiopure aspartic acids featuring conformational lock
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E3 ligand-linker conjugate collection: a promising tool for the discovery of protein degraders
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Scale-up synthesis, stability and physicochemical evaluation of 2,2-difluoro-β-alanine
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Diastereoselective synthesis of 2,3-disubstituted 1,4-dioxanes
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Comprehensive Evaluation of Biochemical Databases in Drug Discovery: Insights from a Crowd-Reviewed Analysis
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α-Spiro-β-prolines – practical access to a rigid molecular platform
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Unexpected TMSCl-promoted reaction of azine carboxamides with aromatic aldehydes
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Handy access to diverse cyclopropanols via cyclopropanation/oxidation sequence of vinyl boronates
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Rawal’s diene-based multigram preparation of spirocyclic pyran building blocks
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Comparison of synthetic routes to decaborane dianion [B
10
H
10
]
2-
– key precursor for carboranes
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Catalytic performance of the Pd-containing hydrogenation catalysts prepared by decomposition of the Pd(0) precursor on various supports
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Paving Rout to Soluble Cage Compounds: in Search for Accessible 2-Heteroadamantanes Source
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Synthesis and stability studies of CF2OMe-decorated aliphatic amines
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Introduction to multistage procedures – another step to qualified synthetic chemist
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Oxazepines fused with another heterocycles by e or f edge
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Nickel Catalysts Prepared by Decomposition of Ni(0) complexeson Activated Carbon for Hydrogenation of Organic Compounds
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Synthesis of conformationally limited δ-amino acidsas a tool for the design of peptide-like foldamers
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Creation of alkyl substituent in α-position of methylene ketones: efficient synthetic toolbox
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Scale-up synthesis of 1-methyladamantane – key precursor to chiral methyl-phenyl-adamantane carboxamide with promising in vitro activity against Ebola virus
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Shelf-stable amino acid derived diazoketones – perspective reagents for medicinal chemistry
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Synthesis and properties of diverse pyrazolines based on flow-generated diazomethanes
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Trifluoromethyl vinamidinium salt – the promising precursor for fused pyridine-contained heterocycles
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2-Oxabicyclo[2.2.2]octane: A New Bioisostere of the Phenyl Ring
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Novel Class of Piperidine Bioisosteres
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Synthesis of 3-Azabicyclo[3.1.1]heptanes
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CF
3
-Diazirines for photoaffinity labeling
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Practical scalable synthesis of N-CF
3
substituted heterocycles
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Unexpected isomerization of oxetane carboxylic acids
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Deoxofluorination of Aliphatic and (Hetero)aromatic Acids
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Convenient Access to Conformationally Rigid Sultams
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Cobalt-containing conducting polymers on carboneous supports for catalytic hydrogenation of quinoline
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Cu-Catalyzed Pyridine Annulation via Oxidative Reaction of Cyclic Ketones with Propargyl Amine
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Expanding of the scope of Castagnoli–Cushman reaction: Anhydrides of cyclic 1,2-dicarbonic acids
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Expanding of the scope of Castagnoli–Cushman Reaction: trifluoracetaldehyde monohydrate
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G3 and G4 Buchwald Precatalysts: Scale up, QC and application for the semi-automated parallel synthesis
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Isoxazole and 1,2,4-Oxadiazole-Derived Phosphonates via [3+2] Cycloaddition
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4,5,6,7-Tetrahydropyrazolo[1,5-a]pyrazine: Lead-oriented scaffold with three diversity points
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Synthesis and reactivity of N-difluoro-cyclopropyl-substituted pyrazoles
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Quick evaluation of catalytic activity of hydrogenation cata-lysts by UV spectra using imidazo[1,5-a]pyridines as probes
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Recent Advances in Difluorocyclopropanation of alkenes using Ruppert–Prakash reagent
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Selective Methylation of α-Methylene Ketones
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Straightforward Synthesis of All Isomeric (Cyclo, fluoro)alkylpiperidines
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Synthesis and properties of monoalkylsubstituted difluorocyclopropenes
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Synthesis of gem-difluorocycloheptanes building blocks
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Difluoro-substituted bicyclo[1.1.1]pentanes (BCPs) for medicinal chemistry
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Novel spirocyclic and fused cyclopropane scaffolds for medicinal chemistry
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Piperazine Bioisosteres for Drug Design
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New Covalent Fragment Libraries by parallel synthesis
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P(O)Me
2
-containing Building Blocks for Drug Design
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Unexpected macrocycles formation in a synthesis of fused aza-cycloalkyl oxazoles
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One-step Synthesis of Functionalized Pyridines by Reaction of Propargylamine and Ketones Catalyzed by Cu(II) Compounds
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Evolution of commercially available compounds for HTS
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Synthesis of medchem-relevant Dimethylphosphine Oxide (DMPO) containing building blocks
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Synthesis of medchem-relevant Dimethylphosphine Oxide (DMPO) containing building blocks
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Catalytic Hydrogenation of Quinoline on Composites of Graphene-like Carbon and 3Dmetals or Their Oxides
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New frontiers in Castagnoli–Cushman Reaction
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An Efficient Approach To Novel Tetrahydropyridoazepines. Expansion Of Azepines’ Drug-like Chemical Space
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Synthesis of Gem-difluorocyclobutane/pentane/hexane Building Blocks – Useful Reagent For Drug Discovery
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Ruppert – Prakash reagent as a difluorocarbene synthetic equivalent for the synthesis of medchem-relevant building blocks
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Cyclobutane ring as a conformational restriction tool
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Saturated Bioisosteres of Benzene with Improved Solubility
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Cubanes for Drug Design
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CH-Activation of L-Proline analogues
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Application of AI to REAL Space: A Step Ahead to Expand the Synthetically Feasible Chemical Space
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Conformationally-rigid pyrrolidines with improved water solubility
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Aminosulfonyl fluorides for drug design
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Difluorocyclopropanes for drug discovery
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Novel spirocycles for drug discovery
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Bicyclic amines for drug discovery by [2+2]-photocyclization
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1,3-Oxazoles and 1,2,4-oxadiazoles as selective agonists of GPR40 receptor
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Design and synthesis of novel 3D-shaped building blocks to “Escape the Flatland”
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Proline analogues: advanced building blocks for drug design
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New synthetic approach to diverse heterocyclic sulfonyl chlorides
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Conformationally restricted scaffolds by Double-Mannich reaction of cyclic ketones
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Synthesis of unique pyrrolidines for drug discovery
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Design and synthesis of morpholine analogues
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Novel fluorinated amines for drug discovery
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CF
3
CHN
2
and C
2
F
5
CHN
2
: highly underestimated reagents
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![Synthesis and Functionalization of Azabicyclo[2.2.1] heptanes for Medicinal Chemistry Applications](/images/posters/Enamine_Synthesis_and_Functionalization_of_Azabicyclo_221_heptanes.png)
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