Pyridone
Intermediate
Summary
Two continuous routes to produce the pyridone intermediate commonly used to prepare Dolutegravir (DTG) are described. The first consists of a two-stage process whereby impurities are purged before the final step to the pyridone is conducted. This process provides the desired product in an overall yield of 86% and a 69-fold enhancement in space-time-yield relative to state of practice processes. The second process is conducted as a through process, continuously from start to finish. The pyridone is common to dolutegravir, cabotegravir and bictegravir and the following report should be of interest to those who manufacture intermediates or active ingredients.
