322407-34-1Relevant articles and documents
Highly regioselective ring-opening of epoxides with amines: A metal- A nd solvent-free protocol for the synthesis of β-amino alcohols
Li, Dong,Wang, Jing,Yu, Shibo,Ye, Silei,Zou, Wenjie,Zhang, Hongbin,Chen, Jingbo
supporting information, p. 2256 - 2259 (2020/03/04)
We herein report a metal- A nd solvent-free acetic acid-mediated ring-opening reaction of epoxides with amines. This process provides β-amino alcohols in high yields with excellent regioselectivity. Importantly, this epoxide ring-opening protocol can be used for the introduction of amines in natural products during late-stage transformations.
THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
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Paragraph 0653; 0656; 0657, (2018/04/26)
The invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein the variables X, Y1-Y5, R1, R2, R3, R4, and Het have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
An improved and efficient process for the scalable preparation of optically pure trans-2-aminocyclohexanols
Xue, Feng,Li, Chang-Gong,Zhu, Yong,Lou, Tian-Jun
, p. 322 - 324 (2014/06/09)
An improved and efficient process has been developed for a green and scalable preparation of optically pure (1R,2R) - and (1S,2S) -trans-2-aminocyclohexanols. The process utilised hot water to promote the aminolysis of cyclohexene oxide by benzylamine to afford racemic trans-2-(benzylamino)cyclohexanols, which were resolved by sequential and repeated use of (R)- and (S)-mandelic acid. Finally, after treatment of the two salts sequentially with HCl and NaOH and recovery of mandelic acid, liberation was achieved of the optically pure trans-2-benzylaminoaminocyclohexanols which were smoothly debenzylated using a low loading of a Pd/C catalyst to the trans-2-aminocyclohexanols. The synthetic route has been successfully applied to large-scale (1 mol) preparations in good yield.