申请人:DAISO CO., LTD.
公开号:EP0930291A1
公开(公告)日:1999-07-21
A process for preparation of 3-amino-2-hydroxy-1-propyl ether of the formula
wherein R1 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic ring, R2 and R3 are the same or different hydrogen atom, a substituted or unsubstituted alkyl, or may form a ring together with an adjacent nitrogen atom, which ring may be interrupted with nitrogen atom, oxygen atom or sulfur atom,
which is characterized in reacting an epoxy compound of the formula
wherein X is halogen,
in the presence of a fluoride salt, with an alcohol and then reacting an amine.
According to the above method, an intermediates for synthesis of medicines is obtained in good yield and highly optical purity.
一种制备式 3-氨基-2-羟基-1-丙基醚的工艺
其中 R1 是取代或未取代的烷基、取代或未取代的芳基或取代或未取代的杂环,R2 和 R3 是相同或不同的氢原子、取代或未取代的烷基,或可与相邻的氮原子一起形成环,该环可被氮原子、氧原子或硫原子打断、
其特征在于使式如下的环氧化合物反应
其中 X 为卤素
的环氧化合物与醇反应,然后与胺反应。
根据上述方法,可以获得产率高、光学纯度高的药物合成中间体。