ECHC 2016

XXVII European Colloquium on Heterocyclic Chemistry

 Amsterdam, The Netherlands    July 3-6, 2016

Programme


14:00

Registration

Session chair:

Prof. Romano ORRU
VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands

16:15

Opening Ceremony

Prof. Vinod SUBRAMANIAM
VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands

16:30

Opening Lecture - PL01 - How Natural Products Can Inspire Chemical Biology and Drug Discovery

Prof. Herbert WALDMANN
MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY, Dortmund, Germany

17:15

Welcome drink - sponsored by MDPI

Session chair:

Dr Eelco RUIJTER
VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands

09:00

IL01 - Fluorinated Imaging Materials

Prof. Tobias RITTER
MAX-PLANCK-INSTITUT FÜR KOHLENFORSCHUNG, Mulheim, Germany

09:35

PL02 - Organocatalytic Asymmetric Synthesis of Heterocycles

Prof. Dieter ENDERS
RWTH AACHEN, Aachen, Germany

10:20

IL02 - The Development of Ligand Systems for Separating Minor Actinides from Lanthanides for Nuclear Fuel Reprocessing

Prof. Laurence HARWOOD
UNIVERSITY OF READING, Reading, United Kingdom

10:55

Coffee break and Exhibition

Session chair:

Prof. Henk HIEMSTRA
UNIVERSITY OF AMSTERDAM, Amsterdam, The Netherlands

11:25

IL03 - Stereoselective Heterocycle Synthesis Coupling Multicomponent Reactions with Biocatalysis or Organocatalysis

Prof. Luca BANFI
UNIVERSITY OF GENOA, Genova, Italy

12:00

IL04 - Metal Free Cllick Reactions For Glycoconjugate Modification

Prof. Geert-Jan BOONS
THE UNIVERSITY OF GEORGIA, Athens, GA, United States

12:35

IL05 - Target Family-Centric Privileged Structures: a Rich Playground for Diverse Heterocyclic Chemotypes

Dr Gerhard MÜLLER
MERCACHEM, Martinsried, Germany

13:10

Lunch, Exhibition and Poster Session 1 (odd numbers)

Session chair:

Prof. Laurence HARWOOD
UNIVERSITY OF READING, Reading, United Kingdom

14:40

Elsevier presentation: Data-Driven Discovery: Deriving and Applying Actionable Information in Medicinal Chemistry

15:00

IL06 - Ynamides: Remarkable Building Blocks for Heterocyclic Synthesis

Prof. Gwilherm EVANO
ULB, Brussels, Belgium

15:35

Start of sessions

Heterocyclic Synthetic Methodology
Heterocyclic Synthetic Methodology
Medicinal Chemistry and Chemical Biology
Heterocyclic Synthetic Methodology
Session chair:
Prof. Laurence HARWOOD
UNIVERSITY OF READING, Reading, United Kingdom
15:35
KL01 - Alpha-Functionalization of Amines as a Tool for the Synthesis of Heterocycles and Natural Products
Prof. Till OPATZ
JOHANNES GUTENBERG-UNIVERSITY, Mainz, Germany
16:00
OC01 - Poxim: A Novel N-Heterocyclic Carbene Equipped with Multifunctional Phosphine Oxide
Prof. Yoichi HOSHIMOTO
FACULTY OF ENGINEERING, OSAKA UNIVERSITY, Suita, Osaka, Japan
16:20
OC02 - Efficient Approach to the Synthesis of 2,3-Substituted Furo[2,3-b]Pyridines
Mr Fernando FUMAGALLI
UNIVERSITY OF SAO PAULO, Ribeirao Preto, Brazil
16:40
Coffee break and Exhibition
17:10
OC03 - Rapid Composition of Spiranoid Lactones: Access to Natural and Unexplored Frames
Dr Dmitry TSVELIKHOVSKY
THE HEBREW UNIVERSITY OF JERUSALEM, Jerusalem, Israel
17:30
OC04 - Nitrosoallenes: Reactivity and Applications to Heterocycles Synthesis
Dr Hiroki TANIMOTO
NARA INSTITUTE OF SCIENCE AND TECHNOLOGY, Nara, Japan
17:50
OC05 - Synthesis of Highly and Diversely Substituted Heterocycles from Alk-3-yn-1-ones (Propargyl Ketones)
Prof. Roman DEMBINSKI
OAKLAND UNIVERSITY, Rochester, MI, United States
Heterocyclic Synthetic Methodology
Session chair:
Prof. Luca BANFI
UNIVERSITY OF GENOA, Genova, Italy
KL02 - First-in-Class MCRs Coupled with Cascade Reactions for the Generation of Molecular Complexity
Prof. Christopher HULME
UNIVERSITY OF ARIZONA, Tucson, United States
OC06 - Asymmetric Synthesis of Natural Tetrahydroisoquinolines and Tetrahydroprotoberberines
Dr Steen INGEMANN JORGENSEN
UNIVERSITY OF AMSTERDAM, Amsterdam, The Netherlands
OC07 - Synthesis of 3-Benzazepines by Metal-Free Oxidative C-H Bond Functionalization-Ring Expansion Tandem Reaction
Mr Andrea GINI
WISSENSCHAFTSZENTRUM STRAUBING, Straubing, Germany
OC08 - Combining Photochemistry and Catalysis: Rapid Access to SP3 - Rich Polyheterocycles from Simple Pyrroles
Ms Emma BLACKHAM
UNIVERSITY OF BRISTOL, Bristol, United Kingdom
OC09 - Intramolecular Tsuji-Trost Cascade Cyclization as a Novel Synthetic Strategy Towards Muironolide A
Mr John BRAUN
VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands
OC10 - C-Brigded N-Heterocycles as New Ligands
Mr Tim-Daniel J. STUMPF
JUSTUS-LIEBIG-UNIVERSITY GIESSEN, Giessen, Germany
Medicinal Chemistry and Chemical Biology
Session chair:
Dr Alessia AMORE
UBIQ, Amsterdam, The Netherlands
KL03 - Biomimetic Natural Product Synthesis
Dr Andrew LAWRENCE
UNIVERSITY OF EDINBURGH, Edinburgh, United Kingdom
OC11 - Pyrazoloquinolinones, Revisited GABAA Receptor Tool Compounds
Mr David Chan Bodin SIEBERT
TU WIEN, Wien, Austria
OC12 - Exploring Tryptophan Synthase as a Herbicidal Mode of Action
Dr Matthew MCLACHLAN
SYNGENTA, Bracknell, Berkshire, United Kingdom
OC13 - The Allylic Azide Rearrangement in Tandem with Huisgen Cycloaddition: Synthesis of Diverse Polyhydroxylated Nitrogen Containing Scaffolds
Ms Rekha CHADDA
SCHOOL OF CHEMISTRY, NUI GALWAY, Galway, Ireland
OC14 - Synthesis and Potential Cytotoxic Activity of New Substituted Indazole Derivatives Bearing Pyrrole and 2-Pyrone
Mr Mohamed EL GHOZLANI
UNIVERSTY SULTAN MY SLIMAN, Béni Mellal, Morocco
OC15 - Towards a Biomimetic Synthesis of Sciodole
Mr Josh HOMER
UNIVERSITY OF AUCKLAND, Auckland, New Zealand
18:10

End of the day

Session Chair:

Dr Tommi MEULEMANS
MERCACHEM-SYNCOM, Nijmegen, The Netherlands

09:00

PL03 - Catalytic Approaches from the Synthesis of Enantiopure Biologically Relevant Heterocycles

Prof. Floris RUTJES
RADBOUD UNIVERSITY NIJMEGEN, Nijmegen, The Netherlands

09:45

PL04 - Carbo- and Heterocycles via Metal-Catalyzed Cycloadditions

Dr Fernando LOPEZ
UNIVERSITY OF SANTIAGO DE COMPOSTELA (USC) AND SPANISH NATIONAL RESEARCH COUNCIL (CSIC), Santiago de Compostela, Spain

10:30

IL07 - Photoactive Molecular and Supramolecular Materials Built-up with Heterocycles

Prof. Gianluca M. FARINOLA
UNIVERSITY OF BARI, Bari, Italy

11:05

Coffee break and Exhibition

Session Chair:

Prof. Huib OVAA
NETHERLANDS CANCER INSTITUTE, Leiden, The Netherlands

11:30

IL08 - Redesigning the Molecules of Nature: Lessons Learned from Total Synthesis

Prof. Karl GADEMANN
UNIVERSITY OF ZÜRICH, Zürich, Switzerland

12:05

IL09 - Copper Catalysis for Synthesis of Enantiopure Alcohols, Amines and Heteroarenes

Prof. Syuzanna HARUTYUNYAN
UNIVERSITY OF GRONINGEN, Groningen, The Netherlands

12:40

IL10 - C-H Functionalization for the Synthesis and Assembly of Heterocycles

Prof. Lutz ACKERMANN
GEORG-AUGUST UNIVERSITY GOETTINGEN, Goettingen, Germany

13:15

Lunch, Exhibition and Poster Session 2 (even numbers)

Session Chair:

Prof. Hermen OVERKLEEFT
LEIDEN UNIVERSITY, Leiden, The Netherlands

14:45

IL11 - Catalysis: A Versatile Tool for the Synthesis of Nitrogen-Containing Heterocycles

Dr Geraldine MASSON
INSTITUT DE CHIMIE DES SUBSTANCES NATURELLES CNRS, Gif-sur-Yvette, France

15:20

Start of sessions

Heterocyclic Synthetic Methodology
Heterocyclic Synthetic Methodology
Medicinal Chemistry and Chemical Biology
Heterocyclic Synthetic Methodology
Session Chair:
Prof. Hermen OVERKLEEFT
LEIDEN UNIVERSITY, Leiden, The Netherlands
15:20
KL04 - New Tricks for Old Heterocycles: from Natural Product Synthesis to Click-Like Functionalizations
Prof. Johan WINNE
UGENT, Ghent, Belgium
15:45
OC16 - Synthesis of Highly Enantioenriched Pyrrolo[1,2-a]Quinolines. Organocatalyzed Domino Cyclopropane Ring Opening/aza-Michael/aldol Reaction Followed by Acid-Promoted Lactamization
Mr Eduardo SANCHEZ
UPV/EHU UNIVERSITY OF THE BASQUE COUNTRY, Leioa, Spain
16:05
OC17 - Brönsted-Acid Catalysed C2-Alkenylation of Aromatic Nitrogen Heterocycles
Mr Giacomo CRISENZA
UNIVERSITY OF BRISTOL, Bristol, United Kingdom
16:25
Coffee break and Exhibition
17:00
OC18 - Rearrangement and Cycloaddition Reactions of Donor-Acceptor Cyclopropanes
Prof. Daniel B. WERZ
TU BRAUNSCHWEIG, Braunschweig, Germany
17:20
OC19 - Pd- and Cu-Catalyzed Stereo- and Regiocontrolled Decarboxylative / C-H Alkenylation of Heroarenes
17:40
OC20 - Enantioselective Organocatalyzed Α-Sulfanylation of Isoxazolidin-5-ones: An Approach To b2,2-Amino Acids
Mr Timothée CADART
LABORATOIRE COBRA UMR 6014, ROUEN, France
Heterocyclic Synthetic Methodology
Session Chair:
Prof. Lutz ACKERMANN
GEORG-AUGUST UNIVERSITY GOETTINGEN, Goettingen, Germany
KL05 - Synthesis of New Spiroacetals by Sustainable Gold Catalysis
Prof. Norbert KRAUSE
DORTMUND UNIVERSITY OF TECHNOLOGY, Dortmund, Germany
OC21 - Is Gold Catalysis a Competitive Method toward Heterocycles ?
Mrs Solčne MIASKIEWICZ
STRASBOURG UNIVERSITY, Strasbourg, France
OC22 - Aliphatic N-Heterocycle Synthesis through Direct C-H Bond Amination
Mr Petrus KUIJPERS
UNIVERSITY OF AMSTERDAM, Amsterdam, The Netherlands
OC23 - 3-Diazoindolin-2-Imines: A Novel Class of Metal Carbene Precursors for the Syntheses of Indole Derivatives
Prof. Yanguang WANG
ZHEJIANG UNIVERSITY, Hangzhou, China
OC24 - Donor-Acceptor Cyclopropanes in Synthesis of Azaheterocycles
Prof. Igor TRUSHKOV
M V LOMONOSOV MOSCOW STATE UNIVERSITY, Moscow, Russia
OC25 - Chirality in Boron-Chelated Dipyrromethene Fluorophores: Synthesis and Chiroptical Investigations
Dr Michael HALL
NEWCASTLE UNIVERSITY, Newcastle upon Tyne, United Kingdom
Medicinal Chemistry and Chemical Biology
Session Chair:
Prof. Henk TIMMERMAN
VU UNIVERSITY AMSTERDAM, Oegstgeest, The Netherlands
KL06 - New Multicomponent Reactions and Strategies to Heterocyclic and Macrocyclic Peptides
Dr Daniel GARCÍA RIVERA
LEIBNIZ INSTITUTE OF PLANT BIOCHEMISTRY / UNIVERSITY OF HAVANA, La Habana, Cuba
OC26 - Palladium-Catalyzed Isocyanide Insertion in Construction of Diverse Heterocycles
Dr Esther VICENTE GARCIA
VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands
OC27 - Biologically Active Indolines - Novel Multi-Functional Indolinic Drugs for the Treatment of Inflammatory Diseases
Prof. Abraham NUDELMAN
BAR ILAN UNIVERSITY, Ramat Gan, Israel
OC28 - Asymmetric Reduction of Enamines towards the Synthesis of (-)-Cytisine and Heterocyclic Building Blocks
Mr Hugo REGO CAMPELLO
UNIVERSITY OF BRISTOL, Bristol, United Kingdom
OC29 - Biology-Oriented Synthesis Based on Privileged Structures: Building Framework Diversity Around Pyrrole Cores
Prof. José Carlos MENÉNDEZ
UNIVERSIDAD COMPLUTENSE, Madrid, Spain
OC30 - Exploring the Antifungal and Antibiofilm Properties of Imidazolium Salts and Fluorescent Benzannulated Benzimidazoles
Prof. Henri SCHREKKER
UNIVERSIDADE FEDERAL DO RIO GRANDE DO SUL, Porto Alegre-RS, Brazil
18:00

End of the day

18:30

Boat tour and Conference dinner

Session Chair:

Prof. Karl Anker JOERGENSEN
AARHUS UNIVERSITY, Aarhus, Denmark

09:00

IL12 - Complex Natural Product as a Driving Force for Discovery in Organic Synthesis and Chemical Biology

Prof. Xiaoguang LEI
PEKING UNIVERSITY, Beijing, China

09:35

IL13 - Metallation–Substitution of Saturated Nitrogen Heterocycles

Prof. Iain COLDHAM
UNIVERSITY OF SHEFFIELD, Sheffield, United Kingdom

10:10

PL05 - Springer Junior Heterocyclic Chemistry Award Lecture (chaired by Bert Maes, editor of Springer)
Exploiting the Reactivity of Strained Rings and Hypervalent Bonds for the Synthesis of Heterocycles

Prof. Jerome WASER
EPFL, Lausanne, Switzerland

10:55

IL14 - α-Perluoroalkylated Cyclic Imines as a Valuable Building Blocks

Prof. Dr Valentine G. NENAJDENKO
MOSCOW STATE UNIVERSITY, Moscow, Russia

11:30

Coffee break and Exhibition

Session Chair:

Prof. Floris RUTJES
RADBOUD UNIVERSITY NIJMEGEN, Nijmegen, The Netherlands

11:55

IL15 - New Strategies for the Synthesis of Heterocyclic through Multicomponent Reactions and Metal-Catalyzed Isomerization

Prof. Thomas NIELSEN
NOVO NORDISK, Copenhagen N, Denmark

12:30

PL06 - Making Molecular Prosthetics with a Small Molecule Synthesizer

Prof. Martin D. BURKE
UNIVERSITY OF ILLINOIS, Urbana, United States

13:15

Lunch

14:15

Start of sessions

Heterocyclic Synthetic Methodology
Enabling Technologies
Medicinal Chemistry and Chemical Biology
Heterocyclic Synthetic Methodology
Session Chair:
Prof. Martin D. BURKE
UNIVERSITY OF ILLINOIS, Urbana, United States
14:15
KL07 - Gamma-Alkylidenebutenolides and Gamma-Hydroxybutyrolactams: Preparation and Reactivity
Dr Laurent COMMEIRAS
AIX-MARSEILLE UNIVERSITY, Marseille cedex 20, France
14:40
OC31 - Picolinic Acid Ligand-Promoted Palladium-Catalyzed C-H Acetoxylation of Simple Arenes
Dr M. Angeles FERNANDEZ-IBANEZ
UNIVERSITY OF AMSTERDAM, Amsterdam, The Netherlands
15:00
OC32 - Stereoselective Transformations of 2h-Chromene Derivatives
Prof. Tibor KURTÁN
UNIVERSITY OF DEBRECEN, Debrecen, Hungary
15:20
Coffee break and Exhibition
15:50
OC33 - Scope and Limitations of the Organocatalyzed Domino Vinylogous Aldol Oxa Michael Reaction
Ms Larissa GEIGER
KARLSRUHE INSTITUTE OF TECHNOLOGY, Karlsruhe, Germany
16:10
OC34 - Dearomative Arylation of Electrophilic Indoles for the Total Synthesis of Natural Products
Prof. Guillaume VINCENT
UNIVERSITÉ PARIS SUD INSTITUT DE CHIMIE MOLÉCULAIRE ET DES MATÉRIAUX D'ORSAY (ICMMO), Orsay, France
16:30
OC35 - Integrative Methodology for Iterative Theory-Experiment Driven Multicomponent Reaction Development
Mr Art KRUITHOF
VU AMSTERDAM, Amsterdam, The Netherlands
Enabling Technologies
Session Chair:
Dr Maikel WIJTMANS
VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands
KL08 - Functionalization of Heterocycles via C–H Activation and Photoredox Catalysis in Batch and Continuous Flow
Dr Timothy NOEL
EINDHOVEN UNIVERSITY OF TECHNOLOGY, Eindhoven, The Netherlands
OC36 - N-Heterocyclic Carbene Ligands in Iridium Complexes for the Detection of Pyridine Analogues in NMR by Non-Hydrogenative Para-Hydrogen Induced Hyperpolarization
Dr Martin FEITERS
RADBOUD UNIVERSITY, Nijmegen, The Netherlands
OC37 - Expansion of the Concept of Nonlinear Effects in Catalytic Reactions Beyond Asymmetric Catalysis
Prof. Michael SCHNÜRCH
TU WIEN, Wien, Austria
OC38 - Direct Heteroatom Incorporating Ester to Arene Transformation: Modular Synthesis of Fluorescent Dyes
Mr Christian FISCHER
UNIVERSITY OF BASEL, Basel, Switzerland
OC39 - Methodology Development Towards the Lasso Peptide Series
Prof. Jan VAN MAARSEVEEN
UNIVERSITY OF AMSTERDAM, Amsterdam, The Netherlands
OC40 - A Lab-Scale Reactor for the Continuous Generation of Anhydrous Diazomethane
Dr Doris DALLINGER
UNIVERSITY OF GRAZ, Graz, Austria
Medicinal Chemistry and Chemical Biology
Session Chair:
Prof. Rob LEURS
VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands
KL09 - Going Beyond ß-Amino Acid Derivatives as Inhibitors of Cathepsin A
Dr Sven RUF
SANOFI-AVENTIS DEUTSCHLAND GMBH, Frankfurt am Main, Germany
OC41 - Designing Residence Time into Heterocyclic Ligands for Drug Targets
Dr Julien LOUVEL
LACDR, Leiden, The Netherlands
OC42 - Photopharmacology
Mr Mickel HANSEN
RIJKSUNIVERSITEIT GRONINGEN, Groningen, The Netherlands
OC43 - Novel Synthesis of Tetrahydroisoquinoline Derivatives Using Petasis Reaction
Dr Agnieszka GRAJEWSKA
ADAM MICKIEWICZ UNIVERSITY, Poznan, Poland
OC44 - Palladium Catalyzed C-Arylation of Amino Acid Derived Hydantoins
Mr Josep MAS ROSELLO
UNIVERSITY OF BRISTOL, Bristol, United Kingdom
OC45 - Enantioselective Synthesis of 4-Arylpyridine Atropisomers by Central-to-Axial Chirality Conversion
Ms Ophélie QUINONERO
ISM2 - INSTITUT DES SCIENCES MOLÉCULAIRE DE MARSEILLE, Marseille, France

Session Chair:

Prof. Romano ORRU
VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands

16:50

PL07 - Organocatalysis for Diversity-Oriented Synthesis

Prof. Karl Anker JOERGENSEN
AARHUS UNIVERSITY, Aarhus, Denmark

17:35

Poster prizes

Prof. Romano ORRU
VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands

17:50

End of the Symposium