A Scalable Synthesis of MN-447, an Antagonist for Integrins αvβ3 and αIIbβ3

…, M Tsushima, D Kubota, Y Yanagisawa…

Index: Ishikawa, Minoru; Tsushima, Masaki; Kubota, Dai; Yanagisawa, Yumiko; Hiraiwa, Yukiko; Kojima, Yasuo; Ajito, Keiichi; Anzai, Naomichi Organic Process Research and Development, 2008 , vol. 12, # 4 p. 596 - 602

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Citation Number: 6

Abstract

(2 S)-Benzenesulfonylamino-3-[3-methoxy-4-{4-(1, 4, 5, 6-tetrahydropyrimidin-2-ylamino) piperidin-1-yl} benzoylamino] propionic acid, MN-447, is a potent antagonist of the integrins αvβ3 and αIIbβ3. Herein, we report a novel synthetic protocol that produces MN-447 in an overall yield of 45%. This protocol, when compared with the original synthetic route for MN- 447, is more cost-effective, requires fewer steps, does not require chromatographic ...