Novel conditions have been developed for the preparation of substituted 2-aminothiophenes employing the Knoevenagel condensation followed by the Gewald reaction. The benefits of these conditions are their mildness, an...Novel conditions have been developed for the preparation of substituted 2-aminothiophenes employing the Knoevenagel condensation followed by the Gewald reaction. The benefits of these conditions are their mildness, and the ease of product isolation. Thus, the Knoevenagel condensation is run in the presence of sodium hydroxide and least amount of ethanol, （in domestic microwave） which combine to perform the roles of desiccant, and catalyst. The Gewald reaction is performed with inorganic base in Ethanol, which suppresses by product formation. This process has been employed in the synthesis of N-nucleosides as a tumor inhibitor.展开更多
文摘Novel conditions have been developed for the preparation of substituted 2-aminothiophenes employing the Knoevenagel condensation followed by the Gewald reaction. The benefits of these conditions are their mildness, and the ease of product isolation. Thus, the Knoevenagel condensation is run in the presence of sodium hydroxide and least amount of ethanol, （in domestic microwave） which combine to perform the roles of desiccant, and catalyst. The Gewald reaction is performed with inorganic base in Ethanol, which suppresses by product formation. This process has been employed in the synthesis of N-nucleosides as a tumor inhibitor.
