Two protocols for the efficient transformation of aromatic as well as aliphatic primary carboxamides to the corresponding carbamates and aromatic as well as aliphatic cyclic imides to the corresponding anthranilic acid derivatives & amino acid derivatives, respectively, are described. We also developed a novel methodology to the multigram scale synthesis of gabapentin and (S)-pregabalin. The gabapentin methyl carbamate was converted to novel potential peptide prodrugs of gabapentin.

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使用DCDMH的一级羧酰胺和环状酰亚胺的霍夫曼重排及其在加巴喷丁及其潜在肽前药合成中的应用

描述了两种有效地将芳族和脂族伯羧酰胺分别有效转化为相应的氨基甲酸酯和将芳族以及脂族环酰亚胺有效转化为相应的邻氨基苯甲酸衍生物和氨基酸衍生物的方案。我们还开发了一种新颖的方法来加巴喷丁和（S）-普瑞巴林的克数合成。加巴喷丁氨基甲酸甲酯被转化为加巴喷丁的新型潜在肽前药。