Synthetic Approaches to the New Drugs Approved During 2020

Abstract

New drugs introduced to the market are privileged structures that have affinities for biological targets implicated in human diseases and conditions. These new chemical entities (NCEs), particularly small molecules and antibody–drug conjugates (ADCs), provide insight into molecular recognition and simultaneously function as leads for the design of future medicines. This Review is part of a continuing series presenting the most likely process-scale synthetic approaches to 44 new chemical entities approved for the first time anywhere in the world during 2020.

Science and claims of the arena of food bioactives: comparison of drugs, nutrients, supplements, and nutraceuticals

“…The biochemical interactions between drugs and targets dictate both their therapeutic effects and toxicity, thus generating a non-linear biological dose–effect correlation. 10…”

“…The pharmaceutical industry looks for and develops highly selective drugs, in terms of unique targets. 10 In short, one molecule, one target, one effect. When medicines do not mimic biological actions, they are usually inhibitors of targets (most often a proteic enzyme).…”

“…The biochemical interactions between drugs and targets dictate both their therapeutic effects and toxicity, thus generating a non-linear biological dose-effect correlation. 10 Molecular biology strongly contributes to the development of 'biological medicines' (often monoclonal antibodies) and small molecules synthesized through drug design based on the target structure. 11 Again, the latter are highly specific (and often inhibitors in nature).…”

Multistep retrosynthesis combining a disconnection aware triple transformer loop with a route penalty score guided tree search

“…35 The commercial process for both drugs was recently reviewed. 36 None of the synthetic steps involved in these two processes occurs in the USPTO dataset used for training TTL, making them a good test case for TTLA. For these examples, we challenged TTLA to predict synthetic routes starting from a list of 534,058 commercially available BB.…”

Reductive Deuteration of Acyl Chlorides for the Synthesis of α,α-Dideuterio Alcohols Using SmI2 and D2O

“…Alcohols are among the most important and broadly utilized building blocks for the synthesis of agrochemicals and drugs [10][11][12][13][14][15][16]. Therefore, deuterium-labeled alcohols are valuable in the preparation of deuterated drugs and deuterated internal standards for agrochemical residue analysis.…”