Citation:
Yin Chen, Yan Zhou, Jun-Hong Li, Jia-Quan Sun, Gui-Sen Zhang. Facile synthesis of suvorexant, an orexin receptor antagonist, via a chiral diazepane intermediate[J]. Chinese Chemical Letters,
;2015, 26(1): 103-107.
doi:
10.1016/j.cclet.2014.09.020
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A facile synthesis of suvorexant, an orexin receptor antagonist, is described. The key intermediate 6 was prepared from R-3-aminobutyric acid through protection, condensation, deprotection, cyclization, and hydrogenation steps. The title product was obtained with a total yield of 31% (>99% ee) after eight linear steps using commercially available raw materials.
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Keywords:
- Synthesis,
- Suvorexant,
- Chiral diazepane
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