Events

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

P04Nahin 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

P06Linda Supe, Ilga Mutule
Synthesis of piperidine-based β-amino alcohols
lindasupe@gmail.com

P07Michał 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

P10William 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)

13.00Opening remarks – Duncan Hay
13.05 - 15.05Session 1 Chair- Andrew Williams
13.05Biocatalysis: An Enabling Tool for the Medicinal Chemist
Sam Staniland, AstraZeneca
13.45Heterobenzylic C-H Functionalisation of Higher Azoles: Strategies for High Productivity and Functional Group Tolerance
Graeme Barker, Heriot Watt University
14.25New functional groups for synthetic and discovery chemistry - Michael Willis, Oxford
15.05Refreshment break
15.20 – 17.00Session 2 Chair- Katherine Jones
15.20-15.40Flash Talk Presentations
15.40Making Difficult-to-Make Molecules: Photochemistry as an Enabling Tool
Susannah Coote, Bath
16.20Photoredox Catalysis for Bioisostere Construction
Olivia Garry, Princeton University
17.00Close

 

Wednesday 24th May 2023 (All times are UK/BST)

13.00 – 15.05Session 3 Chair - Susannah Coote
13.05New molecular motifs and how to make them: N-CF3 and beyond
Franziska Schoenebeck, RWTH Aachen
13.45Synthesizing success: The synthetic chemistry story behind the discovery of DNA polymerase theta chemical probes -
Peter Blencowe, Cancer Research Horizons
14.25A Reaction with Potentional: An Electrosynthesis of 1,3,4-Oxadiazoles from N-Acyl Hydrazones
Luke Chen, University of Strathclyde
15.05Refreshment break
15.30Session 4 Chair – Martin Swarbrick
15.30Process Development of the COVID-19 Oral Protease Inhibitor PF-07321332 at Unprecedented Speed: From Milligrams to Metric Tons in 18 Months
Kaitlyn Gray, Pfizer
16.10Poster Awards
16.15Simplifying Synthesis with Electricity
Phil Baran, Scripps Research Institute
16.55Closing Remarks
17.00Close

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 closed.

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