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Orthogonal validation of NMR fragment hit 27 Encouraged by the relatively high binding affinity of compound 27 compared to expectations for fragments, we synthesised a series of analogues to explore the effect of modifying both the sulfonic acid and the ethoxy substituents on binding affinity (Table 1)

Finally, they were combined, concentrated and freeze-dried to obtain 13.6 g of the finished product, and the purity determined by HPLC was greater than 98%, indicating that this technical condition can be directly scaled up for production

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This work was supported by the Michigan George M

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