A novel and efficient one-pot method has been developed for the synthesis of 1-substituted-3,4-dihydro-β-carbolines from tryptamine and a wide variety of carboxylic acids. The reaction was successfully applied to the synthesis of an important alkaloid harmalan as well as dihydro-eudistomin-U. This represents the first case in which 1-propanephosphonic acid cyclic anhydride (T3P®) has been used in the Bischler–Napieralski reaction. Unexpectedly it was observed that less than two equivalents of the T3P® reagent were sufficient for the two consecutive reactions.

中文翻译：

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T3P®促进的一锅法制备的1取代的3,4-二氢-β-咔啉通过色胺与羧酸反应的合成研究

已经开发了一种新颖有效的一锅法，该方法可从色胺和多种羧酸中合成1-取代的3,4-二氢-β-咔啉。该反应已成功地用于重要的生物碱harmalan以及二氢大黄素-U的合成。这代表了在Bischler-Napieralski反应中使用1-丙烷膦酸环酐（T3P®）的第一种情况。出乎意料的是，观察到少于两个当量的试剂足以进行两个连续的反应。