In small-molecule drug design, saturated heterocycles such as piperidine, piperazine, morpholine, and tetrahydropyran are frequently used because they are structurally stable, their synthetic routes are well established, commercial building blocks are widely available, and they can provide basic ...
If we think of small-molecule drugs as combinations of “functional modules,” N-heterocycles are among the most frequently used modules. A striking change from recent decade-level statistics is that the #1 most frequently occurring N-heterocycle has “passed the baton”—from piperidine to pyridine. ...