公开(公告)号：KR1020090083742A

公开(公告)日：2009-08-04

申请号：KR1020080009722

申请日：2008-01-30

Applicant: 한국기초과학지원연구원 ,  부산대학교 산학협력단

Inventor： 진종성 ,  현명호 ,  정의덕 ,  하현주 ,  조환선 ,  이지연 ,  김태규 ,  신민섭 ,  최희정

IPC: C07D501/20

Abstract: A chiral stationary phase of LC (liquid chromatography) using cefaclor derivative which is an antibiotics suppressing biosynthesis of cell wall is provided to isolate a racemic compound containing a pharmaceutical product having optical activity. A chiral solid phase (CSP1) based on a cepaclo which is cephalosporin based antibiotics is denoted by the chemical formula 1. In the chemical formula 1, R is hydrogen, one or two methyl group, one or two methoxy group or t-butyl group, nitro group, and chloro group. The chiral solid phase(CSP1) ia a novel pirkle chiral solid phase which is applicable to the LC. A method for manufacturing the chiral solid phase of the chemical formula 1 comprises: a step of condensing a compound of the chemical formula 3 with pharmaceutical product having optical activity of the chemical formula 2 to obtain a compound 4; a step of using EEDQ (2-ethoxy-1-ethoxycarbonyl-1,2-dihydroquinoline); and a step of reacting the compound 4 with a silica gel to obtain the chiral solid phase of the chemical formula 1. The chiral column is filled with the chiral solid phase of the chemical formula 1.

Abstract translation: 提供使用头孢克洛衍生物的手性固定相（液相色谱法），其是抑制细胞壁生物合成的抗生素，以分离含有具有光学活性的药物的外消旋化合物。 以化学式1表示基于头孢菌素类抗生素的头孢克罗的手性固相（CSP1）。在化学式1中，R为氢，一个或两个甲基，一个或两个甲氧基或叔丁基 ，硝基和氯基。 手性固相（CSP1）是适用于LC的新型pirkle手性固相。 制备化学式1的手性固相的方法包括：将化学式3的化合物与具有化学式2的光学活性的药物缩合以获得化合物4的步骤; 使用EEDQ（2-乙氧基-1-乙氧基羰基-1,2-二氢喹啉）的步骤; 以及使化合物4与硅胶反应以获得化学式1的手性固相的步骤。手性柱填充有化学式1的手性固相。