Synthesis of 3-Substituted Pyrrolidines via Palladium-Catalyzed Hydroarylation

摘要

class="head no_bottom_margin" id="sec1title">IntroductionSmall molecules with saturated and unsaturated heterocyclic cores are ubiquitous in biochemistry, and much attention has been paid to the manufacture of such structures in academia and industry. Nitrogen-containing saturated rings are particularly privileged structures in biology, and there has therefore been intense interest in the design and use of these heterocycles as drug-like molecules: ca. 60% of the currently US Food and Drug Administration-approved small molecule drugs contain such a motif (). Within the N-heterocycle-containing drug library, the pyrrolidine motif is a very frequently seen structure, and these five-membered rings are widely used in drug discovery, with even relatively simple pyrrolidines often possessing great potency ().Saturated Five-Membered Nitrogen Heterocycles(A) 3-Aryl pyrrolidines are privileged structures, exhibiting powerful effects in a diverse range of biological scenarios, such as leishmaniasis, histone deacetylation, neurotransmission, and gene transcription.(B) 1-Propyl-3-aryl pyrrolidines are potent and selective ligands for serotonin and dopamine receptors.