- 著者
-
的場 勝英
利根 斉
新浜 光一
後藤 文孝
坂 雅之
南川 純一
- 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.407-414, 1999-05-01 (Released:2009-11-16)
- 参考文献数
- 3
- 被引用文献数
-
1
6
An efficient and practical synthetic route to OPC-15161 (1), a novel inhibitor of superoxide anion generation, is described. Intensive survey on pyrazine ring manipulation has led to the development of multi-kilo synthetic pathway, in which beneficial use of a nitrogen protecting group is the key to the problematic cyclization and O-methylation process, both being carried out in one-pot operation. Thus, the synthesis proceeds in 40% overall yield in four steps from tryptophan methyl ester with simple operation and without chromatographic purification, which also opens a general route for the preparation of related 5-alkoxypyrazin-2 (1H) -one 4-oxide such as emeheterone.