【摘 要】
：
近年来,以天然产物L-脯氨酸为原料,通过上保护基、酯化、氨化等步骤,获得BOC-L脯氨,再与苯甲酸与萘酚酸等衍生物在无水无氧条件下和脱保护基合成了新的双活性中心吡咯酰胺化
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近年来,以天然产物L-脯氨酸为原料,通过上保护基、酯化、氨化等步骤,获得BOC-L脯氨,再与苯甲酸与萘酚酸等衍生物在无水无氧条件下和脱保护基合成了新的双活性中心吡咯酰胺化合物。实验结果表明酰胺化的最佳条件是:苯甲酸与萘酚酸衍生物的物质量比为1.5:1,温度25℃,THF为溶剂,通氮气3h,用TFA脱保护基团。
In recent years, natural products of L-proline as raw material, through the protective group, esterification, amination and other steps to obtain BOC-L proline, and then with benzoic acid and naphthol and other derivatives in anhydrous anaerobic Under the conditions and the deprotection of a new biologically active pyrrole compound. The experimental results showed that the optimal conditions for amidation were as follows: the mass ratio of benzoic acid to naphtholic acid derivative was 1.5: 1, temperature was 25 ℃, THF was the solvent, nitrogen was added for 3h, and deprotected with TFA.
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