Fig. 1: Background and introduction to saturated bioisosteres. | Nature Communications

Fig. 1: Background and introduction to saturated bioisosteres.

From: Modular access to saturated bioisosteres of anilines via photoelectrochemical decarboxylative C(sp3)–N coupling

Fig. 1

a Examples of the phenyl bioisosteres core appearing in drugs and bioactive compounds. b The world’s best-selling small molecule drugs containing aniline and diaryl amine motifs. The toxicity of Capesaris associated with the metabolism of aniline could be mitigated by BCP isostere replacement. c Representative saturated bioisosteric scaffolds that faithfully replicate the geometry of substituted anilines. d Typical approaches to amino-bioisosteres from small-ring cage carboxylic acids require pre-activation of carboxylic acids with iodomesitylene diacetate. In this work, a photoelectrochemical decarboxylative platform enables modular access to saturated bioisosteres of anilines.

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