Amide couplings are one of, if not the most common chemical reactions performed in the pharmaceutical industry. Many amide bonds are generated with the help of highly active peptide coupling reagents. These reagents have garnered wide use in the pharmaceutical industry, but many contain high-energy functional groups. As a result, significant time is spent assessing the thermal stability of these reagents before scale-up commences. This paper assesses the thermal stability of 45 common peptide coupling reagents by differential scanning calorimetry and accelerating rate calorimetry. Those compounds which flagged as potentially impact-sensitive or potentially explosive were tested by drop hammer and explosivity screening techniques. The data are presented in an effort to drive the development of these reactions toward the use of one of the more thermally stable reagents.

中文翻译：

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制药行业常用肽偶联剂的热稳定性评估

酰胺偶联是制药工业中最常见的化学反应之一，即使不是最常见的化学反应之一。在高活性肽偶联剂的帮助下会产生许多酰胺键。这些试剂已在制药工业中得到广泛使用，但是许多试剂都含有高能官能团。结果，在开始扩大规模之前，要花费大量时间来评估这些试剂的热稳定性。本文通过差示扫描量热法和加速量热法对45种常用肽偶联剂的热稳定性进行了评估。通过落锤和爆炸性筛选技术对标记为可能具有冲击敏感性或潜在爆炸性的那些化合物进行了测试。