The use of deuterium in the pharmaceutical industry has expanded in recent years as medicinal chemists seek to design compounds with improved and favorable metabolic profiles, hoping to increase the success rate of compounds in the clinic. As a result, process and analytical chemists face new challenges in terms of tracking isotopologues and isotopomers to ensure the quality of intermediates and active pharmaceutical ingredients through manufacture. The work presented herein describes the discovery of an overdeuterated isotopologue, which spurred the development of a simple mitigation strategy. The risk associated with utilizing the overdeuterated isotopologue is examined by kinetic studies of a downstream C–H functionalization reaction.

中文翻译：

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跟踪同位素体：氘代吡唑的合成工艺改进

近年来，随着药物化学家寻求设计具有改善和有利代谢特征的化合物，希望提高化合物在临床上的成功率，氘在制药工业中的使用有所扩大。因此，过程和分析化学家在跟踪同位素异数体和同位素异构体方面面临新的挑战，以确保整个制造过程中中间体和活性药物成分的质量。本文介绍的工作描述了一种超氘同位素体的发现，它促进了一种简单缓解策略的发展。通过下游 C-H 功能化反应的动力学研究检查与使用超氘同位素体相关的风险。