Functionalized Pyridines as Valuable Building Blocks in Organic Synthesis and Medicinal Chemistry

Our Unique Building Blocks to Perform Far and Wide
12 October 2021
Oleg Lukin
Senior Research Scientist

The structural unit of substituted pyridines is present in quite a few widely occurring compounds, including natural products, such as vitamins, coenzymes, and alkaloids, as well as synthetic pharmaceuticals and agrochemicals [1]. As shown in Figure 1, natural compounds containing pyridine rings include nicotinamide 1, pyridoxol (vitamin B6) 2, and the opium alkaloid papaverine 3 used as a muscle relaxant and vasodilator. 

Examples of naturally occurring pyridine derivatives.

Figure 1. Examples of naturally occurring pyridine derivatives.

Pyridine, after piperidine, is the second most common nitrogen heterocycle, appearing in 62 FDA-approved drugs [2-3]. A few examples of the approved pyridine-based drugs are given in Figure 2. In particular, Torasemide 4 in which the pyridine unit is combined with the sulfo urea is an efficient antihypertensive drug. Pyridostigmine 5 is used in the treatment of myasthenia gravis and to reverse the actions of muscle relaxants. Alendronic acid 6 is a bisphosphonate that is a known medication to defeat various forms of osteoporosis, whereas Vismodegib 7 is applied as an anti-carcinoma drug.

Examples of FDA-approved drugs bearing pyridine substructure.

Figure 2. Examples of FDA-approved drugs bearing pyridine substructure.

Shown below are representatives of the pyridine-containing building blocks available from Life Chemicals.

The full list of the functionalized pyridines can be obtained upon request by emailing


  1. (a) Balasubramanian, M.; Keay, J. G. in Comprehensive Heterocyclic Chemistry, 2nd edition, eds. A.R. Katritzky, C.W. Rees, and E.F.V. Scriven, Pergamon, Oxford, 1996. Vol. 5, p. 245. (b) Altaf, A.A.; Shahzad, A.; Gul, Z.; Rasool, N.; Badshah, A.; Lal, B.; Khan, E. J. Drug Design Med. Chem. 2015, 1, 1-11.
  2. Vitaku, E.; Smith, D. T.; Njardarson, J. T. J. Med. Chem. 2014, 57, 10257.
  3. Baumann, M.; Baxendale, I. R. Beilstein J. Org. Chem. 2013, 9, 2265.
12 October 2021, 16:29 Oleg Lukin Building Blocks

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