Table 1. Summary of Stability Data.
Aqueous T1/2 at pH 1.8 determined by 1H NMR. The solution concentrations studied were not sufficient to break the buffer capacity of the system.
Azetidine nitrogen 15N shift.
QM calculated pKa values were determined with Jaguar, version 7.6, Schrodinger, LLC, New York, NY, 2009.
Azetidine nitrogen pKa.
<5% degradation observed at 24 h.
∼50% degradation was observed by the first time point (3–5 min).