A scalable synthesis of MN-447, an antagonist for integrins αvβ3 and αIIbβ 3

Minoru Ishikawa, Masaki Tsushima, Dai Kubota, Yumiko Yanagisawa, Yukiko Hiraiwa, Yasuo Kojima, Keiichi Ajito, Naomichi Anzai

研究成果: Article査読

10 被引用数 (Scopus)

抄録

(2S)-Benzeneslfonylamino-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 αvβ33 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 purification of intermediates and MN-447, and increases the overall yield by 35%. This report focuses on the synthetic strategies that were developed for this protocol. Now, the large quantities of MN-447 that are needed for preclinical and toxicological studies can be readily obtained.

本文言語English
ページ(範囲)596-602
ページ数7
ジャーナルOrganic Process Research and Development
12
4
DOI
出版ステータスPublished - 2008 7月 1
外部発表はい

ASJC Scopus subject areas

  • 物理化学および理論化学
  • 有機化学

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