Electrochemical Synthesis of Substituted Morpholines via a Decarboxylative Intramolecular Etherification
作者:Ryosuke Yamada、Komei Sakata、Takahiro Yamada
DOI:10.1021/acs.orglett.2c00377
日期:2022.3.11
An efficient method for the synthesis of 2,6-multisubstituted morpholines via an electrochemical intramolecular etherification has been developed. The method, which is operationally simple and easy to scale up, provides various substitutedmorpholine derivatives in high yields. The utility of this method is showcased by the synthesis of 2,2,6,6-tetrasubstituted morpholines, which are difficult to synthesize
The invention is related to substituted 2.beta.-morpholino-androstane derivatives, bonded at their 2.beta.-position to the nitrogen of a group of formula I ##STR1## wherein R represents one to four substituents, each one independently selected from (1-4C) alkyl, phenyl and benzyl, or two at the same carbon atom being together --(CH.sub.2).sub.n -- wherein n is 2-6; and Y is O or S, or a pharmaceutically acceptable salt thereof. These steroids are very potent intravenous anaesthetics. The compounds have fast onset times and ideal `sleep duration` vs. `recovery to full coordination` profiles.
The invention is related to substituted 2β-morpholino-androstane derivatives, bonded at their 2β-position to the nitrogen of a group of formula I
wherein R represents one to four substituents, each one independently selected from (1-4C) alkyl, phenyl and benzyl, or two at the same carbon atom being together -(CH₂)n- wherein n is 2-6; and Y is O or S, or a pharmaceutically acceptable salt thereof.
These steroids are very potent intravenous anaesthetics. The compounds have fast onset times and ideal 'sleep duration' vs. 'recovery to full coordination' profiles.
本发明涉及取代的 2β-吗啉-雄甾烷衍生物,其 2β 位与式 I 基团的氮键合
其中 R 代表一至四个取代基,每个取代基独立地选自(1-4C)烷基、苯基和苄基,或两个在同一碳原子上的取代基-(CH₂)n-,其中 n 为 2-6;Y 为 O 或 S,或其药学上可接受的盐。
这些类固醇是非常有效的静脉麻醉剂。这些化合物具有快速起效时间和理想的 "睡眠持续时间 "与 "完全协调恢复 "曲线。