Preparation of Dolutegravir Intermediate Diastereomer

descriptionPublicationkeyboard_double_arrow_right Article 06 Jun 2019 English Publisher:WileyJournal:Journal of Heterocyclic Chemistry, volume 56, pages 2,063-2,067 (issn: 0022-152X, eissn: 1943-5193,

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Authors: Xianheng Wang; Song Chen; Changkuo Zhao; Liangye Long; Yuhe Wang;

doi: 10.1002/jhet.3588

Preparation of Dolutegravir Intermediate Diastereomer

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Abstract

A convenient method was developed to prepare the diastereomer of dolutegravir tricyclic intermediate in the catalysis of EDCI/DMAP in up to 87% yield. Different solvents, temperature, and times were optimized. The synthesized diastereomer 6′ could be used as a standard for the industrial manufacture requirement of dolutegravir active pharmaceutical ingredient.

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Zunyi Medical University
China (People's Republic of)

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