Lemborexant

CAT#: H319647

CAS#: 1369764-02-2

Description: Lemborexant (INN) (code name E-2006, brand name Dayvigo) is a dual antagonist of the orexin OX1 and OX2 receptors which is under development by Eisai for the treatment of insomnia. Lemborexant was approved by the FDA for adults with insomnia in December 2019.

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Synthetic Routes

Lemborexant - Synthetic Route 1

Lemborexant route01

Synthetic reference

Yoshida, Yu; Naoe, Yoshimitsu; Terauchi, Taro; Ozaki, Fumihiro; Doko, Takashi; Takemura, Ayumi; Tanaka, Toshiaki; Sorimachi, Keiichi; Beuckmann, Carsten T.; Suzuki, Michiyuki; Ueno, Takashi; Ozaki, Shunsuke; Yonaga, Masahiro. Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist. Journal of Medicinal Chemistry. Volume 58. Issue 11. Pages 4648-4664. Journal. (2015).

Lemborexant - Synthetic Route 2

Lemborexant route02

Synthetic reference

Terauchi, Taro; Takemura, Ayumi; Doko, Takashi; Yoshida, Yu; Tanaka, Toshiaki; Sorimachi, Keiichi; Naoe, Yoshimitsu; Beuckmann, Carsten; Kazuta, Yuji. Preparation of cyclopropane compounds as orexin receptor antagonists. Assignee Eisai R&D Management Co., Ltd., Japan. WO 2012039371 A1. (2012).