Facile synthesis of suvorexant, an orexin receptor antagonist, via a chiral diazepane intermediate

Yin Chen Yan Zhou Jun-Hong Li Jia-Quan Sun Gui-Sen Zhang

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 shu

Facile synthesis of suvorexant, an orexin receptor antagonist, via a chiral diazepane intermediate

    通讯作者: Gui-Sen Zhang,
摘要: 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.

English

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  • 发布日期:  2014-09-28
  • 收稿日期:  2014-07-08
  • 网络出版日期:  2014-09-05
通讯作者: 陈斌, bchen63@163.com
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