公开(公告)号：KR100453212B1

公开(公告)日：2004-10-15

申请号：KR1020020083097

申请日：2002-12-24

Applicant: 한국과학기술연구원

Inventor： 정찬성 ,  이소하 ,  김영희 ,  채한국 ,  조현성

IPC: C12P41/00

Abstract: PURPOSE: A catalyzed resolution method of racemic cis-1,3-dioxolane derivatives is provided, thereby effectively separating racemic cis-1,3-dioxolane derivatives which is useful as an intermediate used for preparing itraconazole and ketoconazole. CONSTITUTION: The catalyzed resolution method of racemic cis-1,3-dioxolane derivatives represented by formula (1) comprises hydrolysis of racemic cis-1,3-dioxolane derivatives using enzyme in a phosphate buffer solution at pH 6 to 9 and 20 to 60 deg. C to prepare pure cis-1,3-dioxolane derivatives of formulas (1a) and (1b), wherein R is CH2OH, COOH, COOR' or CH2OCOR'; R' is C1-C10 alkyl; the enzyme is Pseudomonas cepacia(PCL) or Candida antartica(CAL).

Abstract translation: 目的：提供外消旋顺式-1,3-二氧戊环衍生物的催化拆分方法，由此有效地分离用作制备伊曲康唑和酮康唑中间体的外消旋顺式-1,3-二氧戊环衍生物。 构成：由式（1）表示的外消旋顺式-1,3-二氧戊环衍生物的催化拆分方法包括使用酶在pH 6至9和20至60的磷酸盐缓冲溶液中水解外消旋顺式-1,3-二氧戊环衍生物 度。 制备式（1a）和（1b）的纯顺式-1,3-二氧戊环衍生物，其中R为CH 2 OH，COOH，COOR'或CH 2 OCOR'; R'是C 1 -C 10烷基; 该酶是洋葱假单胞菌（Pseudomonas cepacia）（PCL）或南极假丝酵母（Candida antartica）（CAL）。

公开(公告)号：KR1020040056592A

公开(公告)日：2004-07-01

申请号：KR1020020083097

申请日：2002-12-24

Applicant: 한국과학기술연구원

Inventor： 정찬성 ,  이소하 ,  김영희 ,  채한국 ,  조현성

IPC: C12P41/00

Abstract: PURPOSE: A catalyzed resolution method of racemic cis-1,3-dioxolane derivatives is provided, thereby effectively separating racemic cis-1,3-dioxolane derivatives which is useful as an intermediate used for preparing itraconazole and ketoconazole. CONSTITUTION: The catalyzed resolution method of racemic cis-1,3-dioxolane derivatives represented by formula (1) comprises hydrolysis of racemic cis-1,3-dioxolane derivatives using enzyme in a phosphate buffer solution at pH 6 to 9 and 20 to 60 deg. C to prepare pure cis-1,3-dioxolane derivatives of formulas (1a) and (1b), wherein R is CH2OH, COOH, COOR' or CH2OCOR'; R' is C1-C10 alkyl; the enzyme is Pseudomonas cepacia(PCL) or Candida antartica(CAL).

Abstract translation: 目的：提供外消旋顺式-1,3-二氧戊环衍生物的催化拆分方法，有效分离外消旋顺式-1,3-二氧戊环衍生物，其用作制备伊曲康唑和酮康唑的中间体。 构成：由式（1）表示的外消旋顺式-1,3-二氧戊环衍生物的催化分解方法包括使用酶在pH6至9和20至60的磷酸盐缓冲溶液中水解外消旋的顺式-1,3-二氧戊环衍生物 度。 制备式（1a）和（1b）的纯的顺式-1,3-二氧戊环衍生物，其中R是CH 2 OH，COOH，COOR'或CH 2 OCOR'; R'是C 1 -C 10烷基; 该酶是洋葱假单胞菌（PCL）或假丝酵母（CAL）。