Development of a Practical and Scalable Synthesis of a Potent p38 Mitogen-Activated Protein Kinase Inhibitor

…, T Kimura, T Takahashi, T Mukuta

Index: Yoshida, Shinya; Obitsu, Kazuyoshi; Hayashi, Yasumasa; Shibazaki, Mitsuyoshi; Kimura, Takenori; Takahashi, Takumi; Asano, Toru; Kubota, Hirokazu; Mukuta, Takashi Organic Process Research and Development, 2012 , vol. 16, # 9 p. 1527 - 1537

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Citation Number: 3

Abstract

Process research and development of a practical and scalable synthetic method toward a potent inhibitor of p38 mitogen-activated protein kinase 1 is described. The medicinal chemistry synthetic method had several issues in scale-up synthesis. In contrast, the synthetic method described here does not require purification by column chromatography for all steps, and the formation of impurities is suppressed well. Aminopyrazole ring formation ...