Reductive Amination in the Synthesis of Pharmaceuticals

Reductive amination plays a paramount role in pharmaceutical and medicinal chemistry owing to its synthetic merits and the ubiquitous presence of amines among biologically active compounds. It is one of the key approaches to C-N bond construction due to its operational easiness and a wide toolbox of protocols. Recent studies show that at least a quarter of C-N bond-forming reactions in the pharmaceutical industry are performed via reductive amination. This Review concisely compiles information on 71 medical substances that are synthesized by reductive amination. Compounds are grouped according to the principle of action, which includes drugs affecting the central nervous system, drugs affecting the cardiovascular system, anticancer drugs, antibiotics, antiviral and antifungal medicines, drugs affecting the urinary system, drugs affecting the respiratory system, antidiabetic medications, drugs affecting the gastrointestinal tract, and drugs regulating metabolic processes. A general synthetic scheme is provided for each compound, and the description is focused on reductive amination steps. The green chemistry metric of reaction mass efficiency was calculated for all reactions. © 2019 American Chemical Society.

Afanasyev O.I.1 , Kuchuk E.1 , Usanov D.L.2 , Chusov D. 1, 3, 4
American Chemical Society
  • 1 A. N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, Vavilova St. 28, Moscow, 119991, Russian Federation
  • 2 Broad Institute, MIT and Harvard, 415 Main Street, Cambridge, MA 02142, United States
  • 3 National Research University Higher School of Economics, Miasnitskaya Str. 20, Moscow, 101000, Russian Federation
  • 4 Peoples' Friendship University of Russia, 6 Miklukho-Maklaya Street, Moscow, 117198, Russian Federation
Antibiotics; Bioactivity; Cardiovascular system; Respiratory system; Biologically active compounds; Bond-forming reactions; Central nervous systems; Gastrointestinal tract; Medical substances; Medicinal chemistry; Pharmaceutical industry; Reductive amination; Amines
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