The present invention relates to a novel method of producing reboxetine diastereomeric derivatives. By reboxetine diastereomeric derivative prepared by the process according to the invention is very excellent in yield, as well as the manufacturing process is simple, performing particularly, the hydroxy group is protected thinner asymmetric-Dihydroxy-alcohol reaction in wheat After introducing oxygen functional groups in stereoselective, after modification of the diol (diol) in the form of a click between sulfate, and enable the die to come at the same time, which are caused by the deprotection process of the protected hydroxy group with a protecting group By clicking sulfate re-arrangement reaction (cyclic sulfate rearrangement) is occurred between the nucleophilic substitution reactions become possible, at this time, but will be a new generation of epoxy reactions have not been reported so far, not accompanied by the same process without further workup in the process In the reaction vessel (one pot) can be performed, and then the synthesis reaction time is shortened by reducing the reaction steps can be produced very efficiently by the reboxetine diastereomeric derivatives, In addition, reboxetine is a serotonin-norepinephrine reuptake inhibiting effect it has according to the present invention reboxetine part thereof diastereomeric derivatives stereoisomers can be useful as depression and attention deficit and hyperactivity disorder (ADHD) pharmaceutical composition for the prevention or treatment.본 발명은 레복세틴 부분입체이성질체 유도체의 신규한 제조방법에 관한 것이다. 본 발명에 의한 제조방법으로 제조된 레복세틴 부분입체이성질체 유도체는 수율이 매우 우수하고, 제조과정이 간단할 뿐만 아니라, 특히, 하이드록시기가 보호된 신나밀알코올에 비대칭 다이히드록시화 반응을 수행함으로써, 산소 작용기를 입체선택적으로 도입한 후, 상기 다이올(diol)을 사이클릭 설페이트의 형태로 변형시킨 후, 상기 다이올을 동시에 활성화하며, 보호기로 보호된 하이드록시기의 탈보호 과정으로 유발되는 사이클릭 설페이트 재배열반응(cyclic sulfate rearrangement)이 일어남으로써, 친핵성 치환반응이 가능해지고, 이때, 지금까지 보고되지 않은 신규의 에폭시 생성반응이 동반될 뿐만 아니라, 이 과정에서 다른 워크업 과정없이 동일 반응용기(one pot)에서 다음반응을 수행할 수 있어 반응 단계가 줄어들어 합성시간이 짧아 매우 효율적으로 레복세틴 부
