3rd Synthesis in Drug Discovery and Development
Event
3rd Synthesis in Drug Discovery and Development
Dates
Tuesday 23rd – Wednesday 24th May, 2023
Place
Virtual (Zoom)
Important links
Twitter hashtag – #SDDD23
Registration link
Posters
Please click the poster number to view the poster
P01 – David Mooney, Ai-Lan Lee, Peter Moore
Direct Minisci-Type C-H Amidation of Purine Bases
dtm2000@hw.ac.uk
P02 – Stuart Smith, Ian Fairlamb, Peter O’Brien
Mechanistic Understanding of Palladium Speciation in Challenging Csp2-Csp3 Suzuki-Miyaura Cross-Couplings (SMCCs)
scs555@york.ac.uk
P03 – W. Felix Zhu, Hanna M. Franz, Claire Empel, Rene M. Königs, Ewgenij Proschak, Victor Hernandez-Olmos
Oxadiazolone-based Pictet-Spengler-type Reaction for the Synthesis of Bioactive and Fluorescent Pyrrole-fused 3-Aminoisoquinolines
zhu@pharmchem.uni-frankfurt.de
P04 – Nahin Kazi, Sarah Allinson, Mark McLaughlin, Susannah Coote
Exploring Cubanes as Bioisosteres for Benzene Rings: Towards the Synthesis of 1,3-Disubstituted Cubanes
s.kazi@lancaster.ac.uk
P05 – Linda Kinena, Daniels Jelisejevs, Edgars Suna
Design and Synthesis of SARS-CoV-2 Mpro Inhibitors Based on Lactam Scaffold
P06 – Linda Supe, Ilga Mutule
Synthesis of piperidine-based β-amino alcohols
lindasupe@gmail.com
P07 – Michał Kamiński,Vittorio Canale, Wojciech Trybała, Jan Rodriguez Parkitna, Paweł Zajdel
Medicinal Mechanochemistry, an efficient and environmentally-friend approach for the synthesis of compound PZ-1190 with potential antipsychotic properties
vittorio.canale@uj.edu.pl
P08 – Joseph Anderson, Nicholas Measom, John Murphy, Darren Poole
Bridge Heteroarylation of Bicyclo[1.1.1]pentane Derivatives
joseph.x.anderson@gsk.com
P09 – Rebecca Stevens, Afjal Miah, Glenn Burley
Multistep HTC-D2B PROTAC Synthesis Enabled by Late-Stage sp2-sp3 Cross-Coupling Chemistry
rebecca.8.stevens@gsk.com
P10 – William Esmieu , Katherine Jones , Daniel Webb, Ryan Tinson , Julian Lewis, James Lewis, Isabelle Lemasson, Giovanni Pinna, Alka Chauhan, Mark Chambers
The Charles River Laboratories PROTAC® Discovery Toolbox: Facilitating the Rapid and Efficient Development of Protein Degraders
daniel.webb@crl.com; ryan.tinson@crl.com
P11 – EV Bedwell, F Emery, G Clososki, I Baxendale, PG Steel
Vectorial Functionalisation of Heterocyclic “Rings of the Future” for Fragment-based Drug Discovery
elizabeth.bedwell@durham.ac.uk
P12 – Ruslan Kotlyarov
Found In Translation: Using Language Models to Predict C–H Borylation Regioselectivity
rk582@cam.ac.uk
P13 – Valentina Noemi Madia, Davide Ialongo, Elisa Patacchini, Merve Arpacioglu, Antonella Messore, Enzo Tramontano, Riccardo De Santis, Florigio Lista, Roberta Costi, Roberto Di Santo
Small molecule derivatives as dual inhibitors of SARS-CoV-2 nsp13 blocking viral replication
valentinanoemi.madia@gmail.com
P14 – Natalia Swiatek, Christine Tran, Chenming Qian, Hossay Abas, Mahesh Mohan, Charlotte Bevan, Alan Spivey
Development and Biological Evaluation of Novel α-Helix Mimetic Prodrugs as Leads for Prostate Cancer Treatment
n.swiatek21@imperial.ac.uk
Synopsis
Synthesis is at the heart of drug discovery and development. The industry has increasingly demanded higher quality clinical candidates and has sought to exploit less druggable biological targets. Densely functionalised small molecules with a high degree of synthetic complexity are often the result of these demands. Successful programmes therefore require the application of innovative synthesis in all stages of discovery and development. The medicinal chemist’s toolbox is also enhanced by the introduction of novel bioisosteres, often made available only through the application of new synthetic methods. This symposium aimed to celebrate the crucial role of synthesis in the success of drug discovery and development.
Programme
Tuesday 23rd May 2023 (All times are UK/BST)
| 13.00 | Opening remarks – Duncan Hay |
| 13.05 - 15.05 | Session 1 Chair- Andrew Williams |
| 13.05 | Biocatalysis: An Enabling Tool for the Medicinal Chemist Sam Staniland, AstraZeneca |
| 13.45 | Heterobenzylic C-H Functionalisation of Higher Azoles: Strategies for High Productivity and Functional Group Tolerance Graeme Barker, Heriot Watt University |
| 14.25 | New functional groups for synthetic and discovery chemistry - Michael Willis, Oxford |
| 15.05 | Refreshment break |
| 15.20 – 17.00 | Session 2 Chair- Katherine Jones |
| 15.20-15.40 | Flash Talk Presentations |
| 15.40 | Making Difficult-to-Make Molecules: Photochemistry as an Enabling Tool Susannah Coote, Bath |
| 16.20 | Photoredox Catalysis for Bioisostere Construction Olivia Garry, Princeton University |
| 17.00 | Close |
Wednesday 24th May 2023 (All times are UK/BST)
| 13.00 – 15.05 | Session 3 Chair - Susannah Coote |
| 13.05 | New molecular motifs and how to make them: N-CF3 and beyond Franziska Schoenebeck, RWTH Aachen |
| 13.45 | Synthesizing success: The synthetic chemistry story behind the discovery of DNA polymerase theta chemical probes - Peter Blencowe, Cancer Research Horizons |
| 14.25 | A Reaction with Potentional: An Electrosynthesis of 1,3,4-Oxadiazoles from N-Acyl Hydrazones Luke Chen, University of Strathclyde |
| 15.05 | Refreshment break |
| 15.30 | Session 4 Chair – Martin Swarbrick |
| 15.30 | Process Development of the COVID-19 Oral Protease Inhibitor PF-07321332 at Unprecedented Speed: From Milligrams to Metric Tons in 18 Months Kaitlyn Gray, Pfizer |
| 16.10 | Poster Awards |
| 16.15 | Simplifying Synthesis with Electricity Phil Baran, Scripps Research Institute |
| 16.55 | Closing Remarks |
| 17.00 | Close |
Who should attend
Chemists from industry and academia, including synthetic, medicinal and process chemists.
Confirmed Speakers
Phil Baran, Scripps Research Institute
Lee Cronin, University of Glasgow
Kaitlyn Gray, Pfizer
Sam Staniland, AstraZeneca
Peter Blencowe, Cancer Research Horizons
Susannah Coote, University of Bath
Michael Willis, University of Oxford
Franziska Schoenebeck, RWTH Aachen
Olivia Garry, Princeton University
Call for Posters / Abstracts
Abstract submission is now closed.
Deadline date for oral submissions is Midnight (GMT), Saturday 31 December 2022.
Deadline date for poster and flash talk submissions is Midnight (GMT), Wednesday 8 March, 2023.
Registration
Registration is now open, please click here to register
Registration Fees
RSC Member* £50.00
Non-Member £80.00
RSC Student** Member* £25.00
Student** Non-Member £40.00
*Member is a paid-up member of the RSC
** Student rates apply to undergraduate and post-graduate students only, but not post-doctoral
Want to become a member?
To join the RSC in order to qualify for discounted registration fees at all RSC, please follow this RSC link.
Exhibitor/Sponsorship Opportunities
Please click here to register your exhibition/sponsorship.
There are two exhibitor packages available to book as follows:
Exhibitor package is priced at £100.00 and includes:
– Name and URL link on BMCS event page
– Rolling slides show at the event and a logo with URL in the electronic handbook
– A4 promotional page in the electronic handbook
Note: no delegate registration is included
Exhibitor plus package is priced at £300.00 and includes:
– Name and URL link on BMCS event page
– Rolling slides show at the event and a logo with URL in the electronic handbook
– A4 promotional page in the electronic handbook
– 3 minute pre-recorded video to be played on loop during the breaks
Note: no delegate registration is included
We are also seeking sponsorship from organisations supporting the low registration fees offered to students. You can support and sponsor this meeting by clicking the booking link above when available.
Confirmed Exhibitors
We are grateful to our confirmed exhibitors for their valued support.
Confirmed Sponsors
We are grateful to our confirmed sponsors for their valued support.
Organising Committee
Duncan Hay (chair), Vertex
Martin Swarbrick (treasurer), Ryvu Therapeutics
Andrew Williams, Hon Chairman, RSC BMCS
Katherine Jones
Secretariat Contact and Further Information
Hg3 Conferences Ltd
+44 (0)1423 529333
E-mail
