ORGN 81 |
A convenient one-pot synthesis of 1,8-naphthyridones
| Shawn A. Springfield, Karen Marcantonio, Scott Ceglia, Jennifer Albaneze-Walker, Peter G. Dormer, Todd D. Nelson, and Jerry A. Murry. Department of Process Research, Merck Research Laboratories, P.O.Box 2000, Rahway, NJ 07065-0900 |
In this manuscript, we disclose an efficient one-pot procedure for the preparation of substituted 1,8-naphthyridin-4-one analogs. Previous efforts to effect this type of transformation were complicated by the formation of benzene tricarboxylate. Via the use of excess base, the impurity formation was completely inhibited. This allowed for the clean preparation of desired intermediate and subsequent formation of naphthyridone analogs in a single flask, which could then be crystallized directly from the reaction mixture in good yield and high purity. |
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