English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Zendy Plus

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Zendy Tools

Zendy Open

GW597599 1 is a novel NK-1 antagonist currently under investigation for the treatment of CNS disorders and emesis. The initial synthetic route devised from the medicinal chemistry one, used several hazardous reagents, gave low yields, and produced high levels of wastes. By targeted process of research and development, application of novel techniques, and extensive route scouting, a novel synthetic route for GW597599 has been developed. This paper reports the optimisation work of the first stage in the chemical synthesis of GW597599: the development of a pilot-plant suitable process for the synthesis of the arylpiperazine derivative 7 in an optically pure fashion. In particular, the process definition allowed eliminating the initial need for cryogenic conditions and copper catalysis in Grignard chemistry. It also allowed replacing a classical resolution step with a more efficient dynamic kinetic resolution, substantially enhancing the overall yield and throughput.

Synthesis of the NK1 Receptor Antagonist GW597599. Part 1: Development of a Scalable Route to a Key Chirally Pure Arylpiperazine