Details

Autor(en) / Beteiligte

• Aoyama, Yasunori
• Hakogi, Toshikazu
• Fukui, Yuki
• Yamada, Daisuke
• Ooyama, Takao
• Nishino, Yutaka
• Shinomoto, Shoji
• Nagai, Masahiko
• Miyake, Naoki
• Taoda, Yoshiyuki
• Yoshida, Hiroshi
• Yasukata, Tatsuro

Titel

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

Ist Teil von

• Organic process research & development, 2019-04, Vol.23 (4), p.558-564

Ort / Verlag

American Chemical Society

Erscheinungsjahr

2019

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• 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.