当前位置: X-MOL 学术Chin. Chem. Lett. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Facile synthesis of suvorexant, an orexin receptor antagonist, via a chiral diazepane intermediate
Chinese Chemical Letters ( IF 9.4 ) Pub Date : 2015 , DOI: 10.1016/j.cclet.2014.09.020
Yin Chen , Yan Zhou , Jun-Hong Li , Jia-Quan Sun , Gui-Sen Zhang

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.

中文翻译:

通过手性二氮杂庚烷中间体轻松合成suvorexant(一种orexin受体拮抗剂)

描述了一种容易合成的食欲素受体拮抗剂suvorexant。关键中间体6R -3-氨基丁酸通过保护,缩合,脱保护,环化和氢化步骤制备。经过八个线性步骤,使用商购可得的原料,获得标题产物,总收率为31%(ee > 99%ee)。
更新日期:2017-01-31
down
wechat
bug