Synthetic toolbox: Amidation

Summary and further reading

In their survey of the reactions used by the pharmaceutical industry in the production of drug candidates, Carey et al.[1] note that not a single catalytic method was used for the synthesis of amides.  There is still a pressing need for scalable catalytic methodologies for the synthesis of amides that are atom efficient and avoid the production of waste; this has encouraged research into the efficient preparation of amide bonds. 

Recommended reading

  • F. K. Ferdousi and A. Whiting, Green Catalytic Direct Amide Bond Formation, in Green and Sustainable Medicinal Chemistry: Methods, Tools and Strategies for the 21st Century Pharmaceutical Industry, The Royal Society of Chemistry, 2016, ch. 13, pp. 156-164.

Details on recent developments in the synthesis of amide bonds can be found in the following reviews:

A specialised review of metal‑catalysed approaches to amide bond formation:

Review of catalytic amide bond formation on non-activated amines and carboxylic acids:

 

  1. J. S. Carey, D. Laffan, C. Thomson and M. T. Williams, Analysis of the reactions used for the preparation of drug candidate molecules, Org. Biomol. Chem., 2006, 4, 2337-2347.