Lucy A. Harwood

Jan 13, 2025 | nature.com | Lucy A. Harwood

A large proportion of FDA-approved drugs contain a nitrogen heterocycle — with the most common being the six-membered aromatic pyridine and its saturated analogue, piperidine. Piperidines often exhibit physicochemical properties, such as solubility and lipophilicity, that afford them an improved pharmacokinetic profile compared with pyridines.

Sep 24, 2023 | dx.doi.org | Jonathan M. E |Lucy A. Harwood |Kirsten Christensen |Ziyue Xiong

Cyclobutyl amino alcohols are versatile synthetic intermediates whose derivatives feature in medicinal chemistry as key components in pharmaceutical candidates, (1) as motifs for exploring QSAR models and in lead/fragment-based drug discovery, (2) and as sp3-rich bioisosteric replacements for their aryl counterparts. (3) Despite this, there are few general methods for producing such compounds, particularly in an enantiomerically enriched form.