MDC Connects: Synthetic chemistry aspects of drug discovery and early development projects
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Presented on 20th May 2020 by James Hitchin, Charnwood Molecular
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MDC Connects: Synthetic chemistry aspects of drug discovery and early development projects
- 1. www.charnwood-molecular.com 1 Excellence in Chemistry
- 2. www.charnwood-molecular.com 2 Chemistry for Drug Discovery Our USPs are our people & our capabilities Innovative Medicinal Chemistry team Highly experienced early PR&D Group Network of strategic Drug Discovery partners Independent, UK-based CRO of over 20 years >60 employees, 85% PhDs International: scientists and clients Synthetic & Medicinal Chemistry expertise
- 3. www.charnwood-molecular.com Synthetic Chemistry Aspects of Drug Discovery and Early Development Projects James Hitchin 3
- 4. www.charnwood-molecular.com 4 Development chemistry Discovery chemistry Fundamentally the same Synthetic chemistry 100s of compounds DMPK Toxicity Underlying biology Phys chem/ drug-like properties Computational chemistry Development chemistry
- 5. www.charnwood-molecular.com 5 Development chemistry Discovery chemistry Fundamentally the same Synthetic chemistry 1 or 2 Compounds Regulatory Requirements Intimate Understanding (DoE) Chemical Engineering Analytical Chemistry Development chemistry
- 6. www.charnwood-molecular.com 6 Baffle - for mixing and temp. sensing StirrerJacket for coolant Carbon steel Sight glass Motor
- 8. www.charnwood-molecular.com 8 Amide bond formation - transformation map UPLC-MS analysis Amide bond formation – case study Recent discovery project
- 9. www.charnwood-molecular.com 9 Beutner Amidation - transformation map Beutner et al. Org. Lett. 2018, 20, 4218−4222 Both products amenable to subsequent SNAr reaction Recent discovery project
- 10. www.charnwood-molecular.com Conclusions • The synthetic considerations of discovery a development chemists are different • Designing your syntheses with an awareness of the challenges of development chemistry could save time and money • Transformation maps provide a detailed understanding of the potential challenges and opportunities in any reaction • Build a transformation map and think about the rate processes driving the different reactions taking place in your flask • Engage each other and work collaboratively to design chemical processes that work efficiently regardless of the stage in the drug discovery process • Thank you for listening! 10
- 11. www.charnwood-molecular.com 11 …for reliable, flexible Drug Discovery Outsourcing from Lead Discovery through to pre-clinical Scale-up Independent, UK-based CRO of 20 years 2 Sites, 40+ employees, 82% PhDs International: scientists and clients Synthetic Organic Chemistry experts Our USPs are our people & our capabilities Innovative Medicinal Chemistry team, from Pharma, Research Institutes & start-ups Big Pharma-experienced early PR&D Group 100% Service business model (FTE or FFS) Network of strategic, expert Drug Discovery partners Excellence in Chemistry
Editor's Notes
- Maybe go for “how do I design out a hERG liability or address and efflux issue” Versus “How do I synthesis 2 Kg of this clinical candidate in the most cost effective, atom economical and environmentally benign manner without using column chromatography Designing compound versus designing synthesis
- Maybe go for “how do I design out a hERG liability or address and efflux issue” Versus “How do I synthesis 2 Kg of this clinical candidate in the most cost effective, atom economical and environmentally benign manner without using column chromatography
- But before we consider the differences between dd and development, we should consider where Lates stage functionalisation for known? Where do they come from?......and the typeof technique has, as you might expect, a pronounced impact on the types of hit you get, which in turn will impact on the complexity of the synthetic strategy. Whatever the case may be, the synthetic strategy is invariable executed in the same way. The type of hit finding platform used will have an impact on the medicinal chemistry strtagey
- Despite some of the differences discussed today, discovery and development chemists share a common background in synthetic chemistry and this is something that they should collaboratively use to their advantage to develop robust processes.