4.5 Article

An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals

Journal

BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
Volume 7, Issue -, Pages 442-495

Publisher

BEILSTEIN-INSTITUT
DOI: 10.3762/bjoc.7.57

Keywords

five-membered rings; heterocycles; medicinal chemistry; pharmaceuticals; synthesis

Funding

  1. Cambridge European Trust
  2. Ralph Raphael Studentship Award
  3. EPSRC
  4. Royal Society
  5. BP endowment
  6. EPSRC [EP/F069685/1] Funding Source: UKRI
  7. Engineering and Physical Sciences Research Council [EP/F069685/1] Funding Source: researchfish

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This review presents a comprehensive overview on selected synthetic routes towards commercial drug compounds as published in both journal and patent literature. Owing to the vast number of potential structures, we have concentrated only on those drugs containing five-membered heterocycles and focused principally on the assembly of the heterocyclic core. In order to target the most representative chemical entities the examples discussed have been selected from the top 200 best selling drugs of recent years.

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