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Simultaneously with our efforts, the Agouron/Lilly groups were investigating 2-methyl benzoyl groups in the P-2 position of their (hydroxyethyl)amine series of inhibitors and had identified the 2-methyl-3-hydroxybenzoyl group in the clinical candidate AG-1343. For leading references to their work see : Kalish, V. J.; Tatlock, J. H.; Davies, J. F., Kaldor, S.W.; Dressman, B.A., Reich, S.; Pino, M.; Nyugen, D.; Appelt, K.; Musick, L.; Wu, B.; Bioorg. Med. Chem. Lett. 1995, 5, 727.
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note
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2 ) we found that after 1 hour at 275°C that the pressure leveled off at 1400 psi and the reaction was done. Isolated yields were ∼70% as in ref. 13a.
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note
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50 values of 1-5 ng/mL and 250-1.0000 ng/mL, respectively.
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85029986430
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note
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