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Late-Stage Functionalization of Drug-Like Molecules Using Diversinates
Christian A Kuttruff1, Margit Haile1, Johannes Kraml1
1Department for Medicinal Chemistry, Boehringer Ingelheim Pharma GmbH & Co KG, Birkendorfer Straße 65, 88397, Biberach an der Riss, Germany.
Chemmedchem
|March 14, 2018
Summary
Late-stage functionalization (LSF) using Baran Diversinates efficiently creates drug analogues. New iron(III) catalysis conditions improve reactions and yield analogues with better drug metabolism and pharmacokinetic (DMPK) properties.
Area of Science:
- Organic Chemistry
- Medicinal Chemistry
- Drug Discovery
Background:
- Late-stage functionalization (LSF) enables rapid analogue generation without de novo synthesis.
- LSF is crucial for optimizing lead compounds in drug discovery pipelines.
Purpose of the Study:
- To apply Baran Diversinates for late-stage functionalization of drug lead structures.
- To accurately predict and achieve desired regioselectivities using computational methods.
- To develop improved LSF conditions for enhanced efficiency and yield.
Main Methods:
- Utilized Baran Diversinates for late-stage functionalization reactions.
- Employed computational methods to predict regioselectivity.
- Developed novel reaction conditions featuring iron(III) catalysis.
- Synthesized new analogues from existing lead structures.
Main Results:
- Successfully achieved specific regioisomers consistent with computational predictions.
- Enhanced reaction conditions led to increased reactivity, reduced reaction times, and improved yields.
- The developed LSF method generated analogues with improved in vitro DMPK parameters.
Conclusions:
- LSF using Baran Diversinates is a viable strategy for rapid analogue synthesis.
- Iron(III) catalysis significantly optimizes LSF reaction efficiency.
- This approach facilitates the discovery of drug candidates with enhanced pharmacokinetic profiles.
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