Fragment-based drug discovery is an important and increasingly reliable technology for the
delivery of clinical candidates. Notably, however, sp3-rich fragments are a largely untapped …

Fragment-based drug discovery (FBDD) has grown and matured to a point where it is
valuable to keep track of its extent and details of application. This Perspective summarizes …

Despite extensive efforts by many practitioners in the field, methods for the direct α‐C− H
bond functionalization of unprotected alicyclic amines remain rare. A new advance in this …

C–H bond functionalization is one of the most effective strategies for the rapid synthesis of
cyclic amines containing substituents on the ring, which are core structures of many …

Polycyclic lactams are prepared in a single operation from o-toluamides and cyclic amines
in a process that involves transient cyclic imines, species that are conveniently obtained in …

Although the C–Hα functionalization of N-heterocycles is, in fact, an easy chemical
transformation, the C–Hβ functionalization is, on the contrary, a quite difficult chemical …

Remote arylation of amines via C–C bond functionalization has not been reported yet.
Herein, we develop the γ-transarylation of amines through the cleavage of unstrained C–C …

A selective Pd‐catalyzed C (3)− H cis‐functionalization of piperidine and tetrahydropyran
carboxylic acids is achieved using a C (4) aminoquinoline amide auxiliary. High mono‐and …

Enolizable cyclic imines, obtained in situ from their corresponding lithium amides by
oxidation with simple ketone oxidants, are readily alkylated with a range of enolates to …

Remote and multiple functionalization of piperidines without the use of transition‐metal
catalysts and elaborate directing groups is one of the major challenges in organic synthesis …