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公开(公告)号：KR1020130088492A
公开(公告)日：2013-08-08
申请号：KR1020120009756
申请日：2012-01-31
Applicant: 한국과학기술연구원
IPC: C07D471/04 , C07D217/04 , A61K31/4375 , A61P25/00
CPC classification number: C07D455/06 , C07F7/0812
Abstract: PURPOSE: A method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ) is provided to simplify a process and to produce a large amount of TBZ or DTBZ. CONSTITUTION: A method for preparing TBZ comprises the steps of: performing alkylation of a compound of chemical formula 3 and a compound of chemical formula 4 to prepare a compound of chemical formula 5; performing aza-prins cyclization of the compound of chemical formula 5 under the presence of an oxidant to prepare a cyclic compound of chemical formula 6; and oxidizing the cyclic compound to convert a methylene group into a keto group and preparing TBZ of chemical formula 1.
Abstract translation: 目的：提供一种制备丁苯那嗪（TBZ）和二氢丁苯那嗪（DTBZ）的方法，以简化工艺并产生大量的TBZ或DTBZ。 构成：制备TBZ的方法包括以下步骤：进行化学式3的化合物和化学式4的化合物的烷基化以制备化学式5的化合物; 在氧化剂存在下进行化学式5的化合物的氮杂稠合环化，制备化学式6的环状化合物; 氧化环状化合物，将亚甲基转化为酮基，制备化学式1的TBZ。
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公开(公告)号：KR101362482B1
公开(公告)日：2014-02-12
申请号：KR1020120009756
申请日：2012-01-31
Applicant: 한국과학기술연구원
IPC: C07D471/04 , C07D217/04 , A61K31/4375 , A61P25/00
CPC classification number: C07D455/06 , C07F7/0812
Abstract: 본 발명은 테트라베나진 (TBZ)과 다이하이드로테트라베나진 (DTBZ)의 제조방법에 관한 것으로, 더욱 상세하게는 6,7-다이메톡시-1,2,3,4-테트라하이드로아이소퀴놀린과 4-메틸-2-(3-(트리메틸실릴)프로프-1-엔-2-일)펜탄을 출발물질로 사용하여, 알킬화 반응, 산화제 존재 하에서의 아자-프린스 고리화 반응, 산화반응을 순차적으로 수행하는 간결하고 짧은 반응공정에 의해 테트라베나진 (TBZ)과 다이하이드로테트라베나진 (DTBZ)을 제조하는 방법에 관한 것이다.
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