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Lead diversification. Application to existing drug molecules: mifepristone 1 and antalarmin 8
M Abid Masood1, Elizabeth Farrant, Inaki Morao
1Worldwide Medicinal Chemistry, Pfizer Worldwide R&D, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. mabidmasood@gmail.com
Abstract:
A series of C-H functionalisation plate-based chemical screens and other C-H activation protocols were developed for the chemical diversification of drug molecules. In this Letter, metalloporphyrin and other catalytic oxidation systems are described in addition to chlorination. Mifepristone and antalarmin are used as substrates. The products obtained and the biological data demonstrate the potential utility of this approach.
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