公开(公告)号：KR1020060025022A

公开(公告)日：2006-03-20

申请号：KR1020040073914

申请日：2004-09-15

Applicant: 한국과학기술연구원

Inventor： 정찬성 ,  이소하 ,  표정인 ,  노관호

IPC: C07D491/048 ,  C07D495/04

Abstract: 본 발명은 유기 전계발광소자용 피리미딘 유도체에 관한 것으로서, 더욱 상세하게는 피리미딘을 모핵으로 하고 여기에 다양한 전자 주게 및 전자 끌게 치환체가 치환되어 있는 신규 구조의 물질로서 청색 발광현상을 나타내므로 유기 전계발광소자로 유용한 피리미딘 유도체에 관한 것이다.
유기 전계 발광소자, 피리미딘 유도체, 유기 OLED.

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）。

公开(公告)号：KR1020040006306A

公开(公告)日：2004-01-24

申请号：KR1020020040324

申请日：2002-07-11

Applicant: 한국과학기술연구원 ,  경동제약 주식회사

Inventor： 정찬성 ,  이소하 ,  문만식 ,  전숙진 ,  이병석

IPC: C07H15/222

Abstract: PURPOSE: A process for preparing Gallamine derivative is provided, thereby cheaply preparing the Gallamine derivative which is useful in synthesis of aminoglycoside antibiotics including isepamycin. CONSTITUTION: A process for preparing Gallamine derivative of the formula(4) comprises the steps of: introducing acetyl(-Ac) or benzyloxycarbonyl(-Cbz) into the amine group of 3,2',6'-NH2 of sisomicin or gentamicin to prepare a compound of the formula(1); reacting the amine group of 1-NH2 of the compound of the formula(1) with anhydride of acid represented by YOH or acid derivative thereof to prepare a compound of the formula(2); introducing acetyl(-Ac) or benzyloxycarbonyl(-Cbz) into the amine group of 3'-NH2 of the compound of the formula(2) to prepare a compound of the formula(3); and reacting the compound of the formula(3) under acid condition to remove purpurosamine or sisosamine ring to prepare the Gallamine derivative of the formula(4), wherein R1 and R2 are independently hydrogen or methyl; X is acetyl or benzyloxycarbonyl; Y is C1 to C10 alkylcarbonyl, or amino or hydroxy substituted C1 to C10 alkylcarbonyl.

Abstract translation: 目的：提供制备Gallamine衍生物的方法，从而廉价地制备可用于合成氨基糖苷类抗生素（包括伊曲霉素）的加仑胺衍生物。 构成：制备式（4）的加仑胺衍生物的方法包括以下步骤：将乙酰基（-Ac）或苄氧羰基（-Cbz）引入西索米星或庆大霉素的3,2'，6'-NH2的胺基中 制备式（1）化合物; 使式（1）化合物的1-NH 2的胺基与由YOH或其酸衍生物表示的酸的酸酐反应以制备式（2）的化合物; 将乙酰基（-Ac）或苄氧羰基（-Cbz）引入式（2）化合物的3'-NH 2的胺基中以制备式（3）化合物; 并在酸性条件下使式（3）的化合物反应以除去嘌呤胺或者sisosamine环以制备式（4）的Gallamine衍生物，其中R 1和R 2独立地是氢或甲基; X是乙酰基或苄氧基羰基; Y为C1至C10烷基羰基，或氨基或羟基取代的C1至C10烷基羰基。

公开(公告)号：KR100341256B1

公开(公告)日：2002-06-21

申请号：KR1019990038839

申请日：1999-09-11

Applicant: 한국과학기술연구원

Inventor： 정찬성 ,  이소하 ,  임대식

IPC: C12P41/00

Abstract: 베라파밀의제조에사용하기위한베라파밀의라세미중간체를가수분해효소를사용하여순수한 (R)- 및 (S)-이성체로분할하는방법및 상기분할된 (R)- 및 (S)-중간체로부터순수한 (R)- 및 (S)-베라파밀을제조하는방법이개시되어있다.

公开(公告)号：KR1020010027210A

公开(公告)日：2001-04-06

申请号：KR1019990038839

申请日：1999-09-11

Applicant: 한국과학기술연구원

Inventor： 정찬성 ,  이소하 ,  임대식

IPC: C12P41/00

Abstract: PURPOSE: Provided is a resolution method of racemic acid precursor of verapamil into (R)- and (S)-enantiomers. And a manufacturing method of pure (R)- and (S)-verapamil therefrom is also provided. The verapamil is a calcium antagonist and thus useful for treatment of hypertension. CONSTITUTION: A resolution method of racemic acid precursor of verapamil is characterized by esterifying racemic acid compound of the formula (1), in the presence of a compound containing acyl group, using hydrolase to resolve (R)- and (S)-enantiomers; hydrolyzing the (R)- and (S)-enantiomers with alcohol; and performing these procedures repeatedly. (R)-(+)- and (S)-(-)-verapamils are manufactured by the steps of: reacting (R)- or (S)- enantiomer with methanesulfonyl chloride or toluenesulfonyl chloride to obtain sulfon derivative; reacting the sulfon derivative with 2-(3,4-dimethoxyphenyl)ethylamine to prepare 2-(3,4-dimethoxyphenyl)ethyl-4-cyano-4-diisopropyl-(3,4-dimethoxyphenyl)butylamine; and methylating 2-(3,4-dimethoxyphenyl)ethyl-4-cyano-4-diisopropyl-(3,4-dimethoxyphenyl)butylamine to obtain pure (R)-(+)- and (S)-(-)-veraphil.

Abstract translation: 目的：提供维拉帕米（R） - 和（S） - 对映异构体的外消旋酸前体的分辨方法。 还提供了纯（R） - 和（S） - 维拉帕米的制造方法。 维拉帕米是钙拮抗剂，因此可用于治疗高血压。 构成：维拉帕米的外消旋酸前体的拆分方法的特征在于在含有酰基的化合物的存在下，使用水解酶分解（R） - 和（S） - 对映异构体，酯化式（1）的外消旋酸化合物。 用醇水解（R） - 和（S） - 对映异构体; 并重复执行这些步骤。 （R） - （+） - 和（S） - （ - ） - 维拉帕米通过以下步骤制备：（R） - 或（S） - 对映体与甲磺酰氯或甲苯磺酰氯反应，得到磺酰衍生物; 使磺酰衍生物与2-（3,4-二甲氧基苯基）乙胺反应制备2-（3,4-二甲氧基苯基）乙基-4-氰基-4-二异丙基 - （3,4-二甲氧基苯基）丁胺; 并将2-（3,4-二甲氧基苯基）乙基-4-氰基-4-二异丙基 - （3,4-二甲氧基苯基）丁胺甲基化得到纯的（R） - （+） - 和（S） - （ - ） - 。

公开(公告)号：KR1019990004221A

公开(公告)日：1999-01-15

申请号：KR1019970028271

申请日：1997-06-27

Applicant: 한국과학기술연구원

Inventor： 김인오 ,  이상기 ,  이소하

IPC: C07C57/38 ,  C07C57/30

Abstract: 본 발명은 다음 화학식 1을 갖는 3,4-디페닐부타노익산 유도체, 그 제조 방법 및 이를 유효 성분으로 하는 살균제 조성물에 관한 것이며,
[화학식 1]

식 중, X는 할로겐 원소, 탄소 1~4개로 이루어진 알킬기, 메톡시기, 페녹시기 또는 브로모페닐기로 이루어진 군 중에서 선택된 것이며, Y는 탄소 1~4개로 이루어진 알킬기가 직접 치환되어 있거나, 탄소 1~4개로 이루어진 알킬기가 치환된 페닐기 또는 할로겐 원소(불소, 염소, 브롬 및 요오드)가 치환된 페닐기이다.