Ethyl 6-chloro-5-cyano-2-methylnicotinate ( 4 ) was coupled with 4-piperidinecarboxylic acid (isonipecotic acid) in 81% yield to pyridine acid 10 . An amide coupling between 10 and benzylsulfonamide ( 6 ) afforded AZD1283 ( 1 ) in 79% yield using CDI as coupling reagent. The synthesis has been developed and scaled up to 20 kg batches of 1, supporting preclinical and clinical studies. Development work towards 2-chloropyridine 4 and benzylsulfonamide ( 6 ) is included.
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Andersen et al. (2013) studied this question.
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