- 著者
- 飯森 隆昌 村井 安 脇坂 康尋 大塚 晏央 大内 章吉 児玉 佳男 大石 武
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.41, no.4, pp.775-777, 1993-04-15 (Released:2008-03-31)
- 参考文献数
- 14
- 被引用文献数
- 2 8
Conformational restrictions of sangivamycin (1) could be achieved by the use of the gauche effect of the substitutents on the ribofranose moiety. The conformational deviations obtained by this method were found to nicely correlate with the inhibitory activity of PKC.
1 0 0 0 OA アミノグリコシド抗生物質アルベカシンの工業的製造法の開発
- 著者
- 飯沼 勝春 村井 安
- 出版者
- The Society of Synthetic Organic Chemistry, Japan
- 雑誌
- 有機合成化学協会誌 (ISSN:00379980)
- 巻号頁・発行日
- vol.57, no.5, pp.368-373, 1999-05-01 (Released:2009-11-16)
- 参考文献数
- 7
- 被引用文献数
- 2 2
Arbekacin, aminoglycoside antibiotic, was synthesized in 1973 by Kondo et al starting from Dibekacin by the acylation of 1-amino group with (S) -4-amino-2-hydroxybutyric acid (AHB), and approved as a chemotherapeutic agent in 1990 limiting to MRSA infection. In the development of industrial large scale synthesis, the main theme was selective protection of four amino groups except 1-amino group. We focused our effort to set up large scale synthetic method by taking advantage of zinc-chelation reaction. By the optimization of reaction conditions and minimization of isolation procedures, final production method was completed. We herein report the development course of high yield and low cost production method by the selective protection of amino group.