Abstract Obtucarbamate A was purified from Disporum cantoniense with good antitussive property. In present work, a series of obtucarbamate A derivatives were designed and synthesized from obtucarbamate A by microwave method, and their antitussive activity were evaluated. The results showed that the toluene diisocyanate was obtained with a yield of 95.1% using a simple method, 1-methyl-2-pyrrolidinone as solvent, temperature of 190 °C, microwave irradiation at 60 W power for 30 min. All compounds have good antitussive activity, and small steric hindrance unsaturated groups of ester chains and amino groups favor activity. It is the first reported of obtucarbamate A derivatives used as antitussive, and the results provide a basis for the application of obtucarbamate derivatives as new antitussive. Graphical Abstract

中文翻译：

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钝氨基甲酸酯A衍生物的合成及镇咳作用

摘要 Obtucarbamate A 是从广州市 Disporum cantoniense 中纯化得到的，具有良好的镇咳作用。在目前的工作中，以obtucarbamate A为原料，通过微波法设计合成了一系列obtucarbamate A衍生物，并对其镇咳活性进行了评价。结果表明，采用简单的方法，以1-甲基-2-吡咯烷酮为溶剂，温度为190 ℃，微波60 W功率照射30 min，得到甲苯二异氰酸酯，产率95.1%。所有化合物均具有良好的镇咳活性，酯链和氨基的空间位阻小不饱和基团有利于活性。首次报道了钝氨基甲酸酯衍生物用作镇咳药，该结果为钝氨基甲酸酯衍生物作为新型镇咳药的应用提供了依据。图形概要