Chemical Communications

Trimethylaluminium mediated amide bond formation in a continuous flow microreactor as key to the synthesis of rimonabant and efaproxiral

T Gustafsson, F Pontén, PH Seeberger

文献索引：Gustafsson, Tomas; Ponten, Fritiof; Seeberger, Peter H. Chemical Communications, 2008 , # 9 p. 1100 - 1102

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被引用次数: 45

摘要

Amide bond formation is a common transformation in medicinal chemistry laboratories. Starting from esters, a three-step sequence of hydrolysis, activation and treatment with an amine is performed. Transfer of this process to larger scale requires further reaction optimization and safety investigations leads to loss in productivity. Aluminium-mediated amine activation is frequently employed to avoid the three step sequence. 18 Trimethylaluminium, the most commonly ...