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公开(公告)号：KR1020040029575A
公开(公告)日：2004-04-08
申请号：KR1020020059879
申请日：2002-10-01
IPC: C07H15/23
Abstract: PURPOSE: A process for producing isepamicin is provided, thereby improving the production yield of isepamicin which is used as an antibiotics via garamine derivatives as an intermediate. CONSTITUTION: A process for producing isepamicin represented by the formula(8) comprises the steps of: introducing acetyl group(-Ac) or benzyloxycarbonyl group(-Cbz) to 3,2',6'-NH2 group of sisomicin or gentamicin to prepare a compound of the formula(1); binding of 1-NH2 group of a compound of the formula(1) with isoserine derivative of the formula(2) to prepare a compound of the formula(3); introducing acetyl group(-Ac) or benzyloxycarbonyl group(-Cbz) to 3'-NH2 group of the compound of the formula(3) to prepare a compound of the formula(4); reacting the compound of the formula(4) under acid condition to remove purpurosamine or sisosamine ring to prepare garamine derivative of the formula(5); reacting the garamine derivative of the formula(5) with glycosyl chloride of the formula(6) to prepare a compound of the formula(7); and reacting the compound of the formula(7) under palladium/carbon catalyst and hydrogen, wherein R1 and R2 are independently hydrogen or methyl; and X is acetyl group(-Ac) or benzyloxycarbonyl group(-Cbz).
Abstract translation: 目的：提供生产异环霉素的方法，从而提高作为中间体的大蒜胺衍生物作为抗生素使用的异环霉素的产率。 构成：由式（8）表示的生产异环霉素的方法包括以下步骤：将乙酰基（-Ac）或苄氧基羰基（-Cbz）引入西索米星或庆大霉素的3,2'，6'- 式（1）的化合物; 式（1）化合物的1-NH 2基团与式（2）的异丝氨酸衍生物的结合以制备式（3）的化合物; 将式（3）化合物的乙酰基（-Ac）或苄氧基羰基（-Cbz）引入3'-NH 2基团以制备式（4）的化合物; 在酸性条件下使式（4）的化合物反应以除去嘌呤胺或者sisosamine环以制备式（5）的甘胺衍生物; 使式（5）的甘胺衍生物与式（6）的糖基氯反应以制备式（7）化合物; 并在钯/碳催化剂和氢气下使式（7）化合物反应，其中R 1和R 2独立地是氢或甲基; X为乙酰基（-Ac）或苄氧基羰基（-Cbz）。
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公开(公告)号：KR100467506B1
公开(公告)日：2005-01-24
申请号：KR1020020059879
申请日：2002-10-01
IPC: C07H15/23
Abstract: PURPOSE: A process for producing isepamicin is provided, thereby improving the production yield of isepamicin which is used as an antibiotics via garamine derivatives as an intermediate. CONSTITUTION: A process for producing isepamicin represented by the formula(8) comprises the steps of: introducing acetyl group(-Ac) or benzyloxycarbonyl group(-Cbz) to 3,2',6'-NH2 group of sisomicin or gentamicin to prepare a compound of the formula(1); binding of 1-NH2 group of a compound of the formula(1) with isoserine derivative of the formula(2) to prepare a compound of the formula(3); introducing acetyl group(-Ac) or benzyloxycarbonyl group(-Cbz) to 3'-NH2 group of the compound of the formula(3) to prepare a compound of the formula(4); reacting the compound of the formula(4) under acid condition to remove purpurosamine or sisosamine ring to prepare garamine derivative of the formula(5); reacting the garamine derivative of the formula(5) with glycosyl chloride of the formula(6) to prepare a compound of the formula(7); and reacting the compound of the formula(7) under palladium/carbon catalyst and hydrogen, wherein R1 and R2 are independently hydrogen or methyl; and X is acetyl group(-Ac) or benzyloxycarbonyl group(-Cbz).
Abstract translation: 目的：提供一种生产异帕米松的方法，由此提高了通过作为中间体的甘氨酸衍生物作为抗生素使用的异扑霉素的产量。 结构式（8）表示的生产异帕米松的方法包括以下步骤：将乙酰基（-Ac）或苄氧基羰基（-Cbz）引入西索米星或庆大霉素的3,2'，6'-NH 2基团以制备 式（1）的化合物; 式（1）化合物的1-NH 2基团与式（2）的异丝氨酸衍生物结合以制备式（3）化合物; 向式（3）化合物的3'-NH 2基团中引入乙酰基（-Ac）或苄氧基羰基（-Cbz）以制备式（4）化合物; 在酸性条件下使式（4）化合物反应除去紫苏糖胺或sisosamine环，制备式（5）的甘氨酸衍生物; 使式（5）的甘氨酸衍生物与式（6）的糖基氯反应以制备式（7）的化合物; 和使式（7）化合物在钯/碳催化剂和氢气下反应，其中R1和R2独立地为氢或甲基; X是乙酰基（-Ac）或苄氧基羰基（-Cbz）。
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Patent Agency Ranking
公开(公告)号：KR100842944B1
公开(公告)日：2008-07-02
申请号：KR1020070056892
申请日：2007-06-11
Applicant: 한국과학기술연구원
CPC classification number: C12P19/02
Abstract: A method for preparing ribofuranoside having a hydroxy group at C5 position is provided to save energy and be environment-friendly using an enzyme reaction, thereby being effective for constructing molecular diversity and synthesizing a precise compound. To prepare ribofuranoside having a hydroxy group at C5 position, (C1-6 alkyl)-2,3,5-tri(C1-6 alkanoyl)ribofuranoside represented by a formula(1) as a substrate is hydrolyzed at the C5 position selectively by an enzyme selected from the group consisting of lipase derived from Pseudomonas fluorescence, lipase derived from Burkholderia cepacia, lipase derived from Pseudomonas cepacia, acylase derived from Aspergillus sp., PLE(pig liver esterase), LWG(wheat germ lipase), lipase derived from Bacillus thermoleovorans, Amano lipase M and lipase derived from Alcaligenes sp., wherein the substrate is beta methyl 2,3,5-triacetyl ribofuranoside or beta methyl 2,3,5-tripropionyl ribofuranoside. In the formula(1), R^1 is C1-6 alkyl and R is C1-6 alkanoyl.
Abstract translation: 提供了一种在C5位置具有羟基的呋喃核糖苷的制备方法，以便利用酶反应来节约能源并使其环境友好，从而有效地构建分子多样性并合成精确的化合物。 为了制备在C5位具有羟基的呋喃核糖苷，通过式（1）表示的（C 1-6烷基）-2,3,5-三（C 1-6烷酰基）呋喃核糖核苷作为底物，在C5位选择性地水解 选自源自假单胞菌荧光的脂肪酶，源自洋葱伯克霍尔德菌的脂肪酶，源自洋葱假单胞菌的脂肪酶，源自曲霉属的酰基酶，PLE（猪肝酯酶），LWG（小麦胚芽脂酶）），源自 嗜热脂肪芽孢杆菌，天牛脂肪酶M和源自产碱杆菌属的脂肪酶，其中底物是β甲基2,3,5-三乙酰基呋喃核糖苷或β甲基2,3,5-三丙酰基呋喃核糖苷。 式（1）中，R 1为C 1-6烷基，R为C 1-6烷酰基。
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公开(公告)号：KR1020080014485A
公开(公告)日：2008-02-14
申请号：KR1020060076272
申请日：2006-08-11
Applicant: 한국과학기술연구원
IPC: C07D239/96
Abstract: A regioselective reduction method of quinazolin-2,4-dione derivatives is provided to synthesize new chemical library, obtain a molecular skeleton having new biological activity useful for screening a compound having new medicinal efficacy, and allow acquisition of molecular diversity for the compounds. The carbonyl group at C2 and C4 sites of quinazolin-2,4-dione derivatives represented by the formula(1) is regioselectively reduced to methylene group by using a reducing agent such as aluminum or boron derivatives, a reaction solvent of tetrahydrofuran at atmosphere pressure and -20 deg. C to reflux temperature of solvent, wherein R1 is hydroxy group, C1-C6 alkoxy group, amine group or C1-C6 alkylamine group; R2 is hydrogen atom, C1-C6 alkyl group, phenyl group, benzyl group or halogen-substituted benzyl group.
Abstract translation: 提供了喹唑啉-2,4-二酮衍生物的区域选择性还原方法，以合成新的化学文库，获得具有新的生物活性的分子骨架，可用于筛选具有新药物功效的化合物，并且可以获得化合物的分子多样性。 式（1）表示的喹唑啉-2,4-二酮衍生物C2和C4位置上的羰基通过使用还原剂如铝或硼衍生物，四氢呋喃在大气压下的反应溶剂区域选择性地还原成亚甲基 和-20度。 C至溶剂的回流温度，其中R1为羟基，C1-C6烷氧基，胺基或C1-C6烷基胺基; R2是氢原子，C1-C6烷基，苯基，苄基或卤素取代的苄基。
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公开(公告)号：KR100450607B1
公开(公告)日：2004-09-30
申请号：KR1020020040324
申请日：2002-07-11
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：提供了一种制备Gallamine衍生物的方法，由此便宜地制备了用于合成氨基糖苷类抗生素（包括异阿霉素）的Gallamine衍生物。 构成：制备式（4）的Gallamine衍生物的方法包括以下步骤：将乙酰基（-Ac）或苄氧基羰基（-Cbz）引入西索米星或庆大霉素的3,2'，6'-NH 2的胺基中， 制备式（1）的化合物; 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; 在式（2）化合物的3'-NH 2的胺基中引入乙酰基（-Ac）或苄氧基羰基（-Cbz）以制备式（3）的化合物; （3）的化合物在酸性条件下反应以除去紫苏糖胺或sisosamine环以制备式（4）的Gallamine衍生物，其中R 1和R 2独立地为氢或甲基; X是乙酰基或苄氧基羰基; Y是C1至C10烷基羰基，或氨基或羟基取代的C1至C10烷基羰基。
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公开(公告)号：KR100844192B1
公开(公告)日：2008-07-04
申请号：KR1020060076272
申请日：2006-08-11
Applicant: 한국과학기술연구원
IPC: C07D239/96
Abstract: 본 발명은 퀴나졸린-2,4-디온 유도체의 위치선택적 환원방법에 관한 것으로서, 더욱 상세하게는 방향족 이환기(aromatic heterocyclic compound)를 갖는 화합물로서 분자 구조내에 카르복시산, 에스터, 아마이드 및 우레아와 같은 카르보닐 기능기가 다수 포함되어 있는 다음 화학식 1로 표시되는 퀴나졸린-2,4-디온 유도체에서 특정 위치의 카르보닐기를 선택적으로 환원 반응하여 메틸렌기로 전환하는 방법에 관한 것이다.
상기 화학식 1에서, R
1 은 하이드록시기, C
1 -C
6 알콕시기, 아민기, 또는 C
1 -C
6 알킬아민기를 나타내고, R
2 는 수소원자, C
1 -C
6 알킬기, 페닐기, 벤질기, 또는 할로겐 치환된 벤질기를 나타낸다.
퀴나졸린, 환원반응, 환원제, 반응선택성, 위치선택성, 신약, 화합물 군-
公开(公告)号：KR1020040006306A
公开(公告)日：2004-01-24
申请号：KR1020020040324
申请日：2002-07-11
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。
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