Despite the apparent simplicity of forming amide bonds, the compendium of literature describing amide coupling reagents and methodologies still continues to grow. The presence of active research in this field alludes to underlying complexities of amide bond synthesis – perhaps not so much in the bond itself, but in practical aspects such as solubility, post-reaction purification, and the reactivity of activated intermediates.<br/><br/>These issues are particularly pronounced in the pharmaceutical industry where strict impurity control and predictability are required, and can be challenging to overcome. A few recent examples highlighting innovative approaches, such as kinetic modeling and statistical analyses, to solve these problems in a cost- and time-efficient manner are described.

Application of mechanistic modeling to facilitate API process development

253rd National Meeting (2017)

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