Synthetic Route Design of AZD4635, an A2AR Antagonist

The AstraZeneca approach to synthetic Route Design is exemplified through our AZD4635 chemical development program. The identification of possible new route concepts is presented, as well as their subsequent prioritization for practical exploration based on project objectives. Selected ideas were tested to demonstrate proof of concept for the bond formation strategy and, where successful, were fed into a decision tool based on key SELECTion principles.

• Mairi M. Littleson ^*†, Andrew D. Campbell ^†, Adam Clarke ^†, Mark Dow ^†, Gareth Ensor ^†, Matthew C. Evans ^†, Adam Herring ^†,Bethany A. Jackson ^†, Lucinda V. Jackson ^†, Staffan Karlsson ^‡, David J. Klauber ^†, Danny H. Legg ^§, Kevin W. Leslie ^†, Štefan Moravcí̌k ^‡, Chris D. Parsons ^§, Thomas O. Ronson ^†, Rebecca E. Meadows ^†

• ^† Chemical Development, Pharmaceutical Technology and Development, AstraZeneca, Macclesfield Campus, SK10 2NA, Macclesfield, U.K.
• ^‡ Early Chemical Development, Pharmaceutical Sciences, IMED Biotech Unit, AstraZeneca, Gothenburg, SE-431 83 Mölndal, Sweden
• ^§ Early Chemical Development, Pharmaceutical Sciences, IMED Biotech Unit, AstraZeneca, Macclesfield Campus, SK10 2NA, Macclesfield, U.K.

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