Practical and Scalable Synthetic Method for Preparation of Dolutegravir Sodium: Improvement of a Synthetic Route for Large-Scale Synthesis

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Abstract Image

A practical and scalable synthetic method to obtain dolutegravir sodium (1) was established starting from the readily accessible material maltol (2). This synthetic method includes a scalable oxidation process of maltol and palladium-catalyzed amidation for introduction of an amide moiety, leading to a practical manufacturing method in short synthetic steps. The synthetic method demonstrated herein enables multikilogram scale manufacturing of 1 of high purity.

Practical and Scalable Synthetic Method for Preparation of Dolutegravir Sodium: Improvement of a Synthetic Route for Large-Scale Synthesis

 API R&D Laboratory, CMC R&D DivisionShionogi and Co., Ltd.1-3, Kuise Terajima 2-chome, Amagasaki, Hyogo 660-0813, Japan
 Production Technology Department, Manufacturing DivisionShionogi and Co., Ltd.1-3, Kuise Terajima 2-chome, Amagasaki, Hyogo 660-0813, Japan
§ Shionogi Pharmaceutical Research CenterShionogi and Co., Ltd.1-1, Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan
Org. Process Res. Dev., Article ASAP
DOI: 10.1021/acs.oprd.8b00409
Publication Date (Web): March 1, 2019
Copyright © 2019 American Chemical Society
This article is part of the Japanese Society for Process Chemistry special issue.

https://pubs.acs.org/doi/10.1021/acs.oprd.8b00409

///////Dolutegravir

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