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Paper | Regular issue | Vol 94, No. 5, 2017, pp.938-948
Published online, 26th April, 2017
DOI: 10.3987/COM-17-13700
An Efficient and Practical Method for the Synthesis of the 5-Acylamino-4-(4-pyrimidinyl)isoxazole Derivative AKP-001, a Potent P38 MAP Kinase Inhibitor

Shuji Ohta,* Takahisa Saito, Jun-ya Kato, Shuichiro Sato, Hiroyuki Hayashi, and Koichi Hasumi

*Synthetic Research Department, ASKA Pharmaceutical Co., Ltd., 5-36-1, Shimosakunobe, Takatsu-ku, Kawasaki-shi, Kanagawa 213-8522, Japan


5-Acylamino-4-(4-pyrimidinyl)isoxazole derivative AKP-001 is a p38 mitogen-activated protein kinase inhibitor previously developed in our laboratory as an anti-inflammatory agent. Herein, we report our studies leading to the development of an improved synthetic route to AKP-001, which shows several advantages compared to the previously reported laboratory-scale process, namely, a lower number of steps, superior chemical yield and atom efficiency, and applicability at an industrial scale.