Fragment-based drug discovery enables translation of novel (3D) chemistries into biologically relevant hit matter, as demonstrated by the identification and optimization of a cyclobutane-based 3D fragment into a potent histamine H1 receptor ligand.
Kinetic resolution of spirocyclic 2-arylpiperidines was achieved with sparteine as a chiral ligand.
A transition metal-free strategy for the α,β-C(sp3)–H dehydrogenative diazotization of piperidines has been developed. This method proceeds at room temperature under air, eliminating stoichiometric external oxidants and harsh conditions.
In the last decade numerous techniques have been developed in Pd-catalysed distal C–H activation ranging from template-assisted to the use of inherent functional groups as the directing auxiliary including ligand-enabled transformations.
A chemodivergent organolithium-mediated protocol to promote anionic Fries rearrangement (AoF) or kinetic resolution (KR) processes starting from O-aryl carbamates of 2-substituted piperidines is reported.