The Curtius rearrangement is the thermal decomposition of an acyl azide derived from carboxylic acid to produce an isocyanate as the initial product. The isocyanate can undergo further reactions to provide amines and their derivatives. Due to its tolerance for a large variety of functional groups and complete retention of stereochemistry during rearrangement, the Curtius rearrangement has been used in the synthesis of a wide variety of medicinal agents with amines and amine‐derived functional groups such as ureas and urethanes. The current review outlines various applications of the Curtius rearrangement in drug discovery and medicinal chemistry. In particular, the review highlights some widely used rearrangement methods, syntheses of some key agents for popular drug targets and FDA‐approved drugs. In addition, the review highlights applications of the Curtius rearrangement in continuous‐flow protocols for the scale‐up of active pharmaceutical ingredients.

中文翻译：

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Curtius重排：在现代药物发现和药物化学中的应用

库尔修斯重排是衍生自羧酸的酰基叠氮化物的热分解，以产生作为初始产物的异氰酸酯。异氰酸酯可进行进一步反应以提供胺及其衍生物。由于其对多种官能团的耐受性以及在重排过程中完全保留立体化学，因此Curtius重排已用于合成多种具有胺和胺衍生的官能团（例如尿素和尿烷）的药物。本综述概述了库尔修斯重排在药物发现和药物化学中的各种应用。尤其是，本综述重点介绍了一些广泛使用的重排方法，一些用于流行药物靶标的关键药物的合成以及FDA批准的药物。此外，