-
-
公开(公告)号：KR100761773B1
公开(公告)日：2007-10-04
申请号：KR1020060066203
申请日：2006-07-14
Applicant: 한국화학연구원
IPC: C07D493/08
Abstract: A method for preparing brevicomin and a derivative thereof is provided to synthesize isomers of the brevicomin stereo-selectively and efficiently by using an organic catalyst of an L-proline or D-proline and a Hoveyda-Grubbs catalyst. A method for preparing four kinds of isomers of brevicomin or derivatives thereof represented by the formula(1) comprises the steps of: (a) after reacting nitroso-benzene(Ph-NO) with an aldehyde(R1CHO) in the presence of an L- or D-proline catalyst, reacting it with an allyl halide to prepare a compound represented by the formula(2); (b) reacting the compound of the formula(2) in the presence of a copper salt catalyst such as copper acetate and copper sulfate to prepare a diol compound represented by the formula(3); (c) reacting the compound of the formula(3) with a vinyl ketone(R2COCHCH2) in the presence of a Hoveyda-Grubbs catalyst to prepare a compound represented by the formula(4); and (d) treating the compound of the formula(4) with an inorganic acid such as HCl in the presence of a Pd/C catalyst under the hydrogen pressure. In the formulae, each R1 and R2 is independently C1-10 alkyl, allyl or alkyl allyl group.
Abstract translation: 提供一种制备短纤维素及其衍生物的方法，通过使用L-脯氨酸或D-脯氨酸和Hoveyda-Grubbs催化剂的有机催化剂，立体选择性和有效地合成短纤维的异构体。 制备由式（1）表示的四种或其衍生物的四种异构体的方法包括以下步骤：（a）在L存在下使亚硝基苯（Ph-NO）与醛（R1CHO）反应后， - 或D-脯氨酸催化剂，使其与烯丙基卤反应，制备由式（2）表示的化合物; （b）在铜盐催化剂如乙酸铜和硫酸铜存在下使式（2）化合物反应，制备由式（3）表示的二醇化合物; （c）在Hoveyda-Grubbs催化剂存在下使式（3）的化合物与乙烯基酮（R 2 COCHCH 2）反应，以制备由式（4）表示的化合物。 和（d）在Pd / C催化剂存在下，在氢气压力下，用无机酸如HCl处理式（4）的化合物。 在该式中，R 1和R 2各自独立地为C 1-10烷基，烯丙基或烷基烯丙基。
-
公开(公告)号：KR100589429B1
公开(公告)日：2006-06-14
申请号：KR1020040068860
申请日：2004-08-31
Applicant: 한국화학연구원
IPC: C07D401/04
Abstract: 본 발명은 N-1 위치에 아미노피리딜기가 치환된 퀴놀론 유도체를 제조하는 방법에 관한 것으로, 본 발명에 따라 3-옥소-프로피온산 에틸 에스테르 유도체와 트리에틸오르소포메이트의 반응으로 생성된 에톡시에틸렌 유도체에 2-아미노-3,5,6-트리플루오르피리딘을 도입시킨 후 이를 고리화하고 아미노기를 도입시키는 단계를 포함하는 하기 화학식 1의 N-1 위치에 3,5-다이플루오르-6-아미노피리딜기가 치환된 퀴놀론 유도체 제조 방법은, 산업적 적용이 용이한 공정을 통해 N-1 위치에 3,5-다이플루오르-6-아미노피리딜기가 치환된 퀴놀론 유도체를 고수율로 제조할 수 있으므로 CCR(cellular chemokine receptor: 세포화학수용체)5 모듈레이터(modulator)의 제조 뿐만 아니라 감염증 치료제(anti-infective agents)의 제조 등에 유용하게 활용될 수 있다.
상기 식에서, R
1 은 수소, 아미노 또는 메틸이고; R
2 는 불소, 염소, 메틸아미노, 2-하이드록시에틸아미노, N-메틸-N-(2-하이드록시에틸)아미노, 2-메톡시에틸 아미노 또는 (피롤리딘-3-일)아미노이며; W는 CH, N, CF, CCl, CBr, COCH
3 또는 CCH
3 이다.Abstract translation: 本发明涉及一种用于生产喹诺酮衍生物取代的氨基是吡啶基的N-1位置上，按照本发明，3-氧代 - 丙酸酯衍生物和由攀登包伴侣乙氧基乙烯的反应中产生的三乙基甲硅烷 3,5-氟-6-氨基-2-氨基-N-1式1的位置，其中包括环化它的在衍生物引入后3,5,6-三氟 - 吡啶步骤和导入氨基 该方法的槽纹莳萝基团被取代的喹诺酮衍生物，因此工业应用可以以高收率由一个简单的方法制备，3,5-氟-6-氨基嘧啶吡啶基被取代的CCR的N-1位置的喹诺酮衍生物 它可以用于生产抗感染剂以及制造细胞趋化因子受体调节剂（5）。
-
公开(公告)号：KR1020040058612A
公开(公告)日：2004-07-05
申请号：KR1020020084961
申请日：2002-12-27
Applicant: 한국화학연구원
IPC: C07D207/26
Abstract: PURPOSE: A method for preparing 4-hydroxy-2-pyrrolidinone is provided, thereby removing additional purification process that uses excessive solvent or excessive ammonia in a high pressure reactor, and easily preparing 4-hydroxy-2-pyrrolidinone with high purity in higher yield. CONSTITUTION: The method for preparing 4-hydroxy-2-pyrrolidinone represented by formula (1) comprises the steps of: (1) amide reacting a compound of formula (2) with a compound of formula (3) to prepare a compound of formula (4); (2) cyclization reacting and decarbonating the compound of formula (4) to prepare diketo intermediate, and reducing the diketo intermediate to prepare a compound of formula (5); and (3) reacting the compound of formula (5) with protonic acid, wherein R1 and R2 are independently C1-C4 alkyl or alkenyl; R3 is ethyl or propyl with phenyl substituted with phenyl, naphtyl, methoxy, nitro or halogen at the C-1 site, 2-hydroxyethyl, 2-aminoethyl, or 2-phenylethyl; and X is hydroxide or halogen atom.
Abstract translation: 目的：提供一种制备4-羟基-2-吡咯烷酮的方法，从而除去在高压反应器中使用过量溶剂或过量氨的附加纯化方法，并以更高的产率容易地制备高纯度的4-羟基-2-吡咯烷酮 。 构成：由式（1）表示的制备4-羟基-2-吡咯烷酮的方法包括以下步骤：（1）将式（2）化合物与式（3）化合物酰胺反应，制备式 （4）; （2）使式（4）的化合物进行环化反应并脱碳以制备二酮中间体，还原二酮中间体以制备式（5）化合物; 和（3）使式（5）的化合物与质子酸反应，其中R 1和R 2独立地为C 1 -C 4烷基或链烯基; R3是乙基或丙基，苯基，萘基，甲氧基，硝基或卤素被C-1位取代的苯基，2-羟乙基，2-氨基乙基或2-苯基乙基; X为氢或卤原子。
-
公开(公告)号：KR100424393B1
公开(公告)日：2004-03-24
申请号：KR1020010073696
申请日：2001-11-26
Applicant: 한국화학연구원
IPC: C07D207/12
Abstract: PURPOSE: A method of preparing oxiracetam is provided to make oxiracetam product in high purity and yield. The oxiracetam improves brain functions and therapeutic effect on dementia. CONSTITUTION: In a method of preparing oxiracetam of the formula(1), a tri-amide compound of the formula(2) is first prepared by reacting an organic solvent compound of the formula(4) with an organic solvent compound of the formula(5). A compound of the formula(3) is prepared by sequentially conducting cyclization, decarboxylation and reduction with respect to the compound of the formula(2). The compound of the formula(3) reacts with ammonia under the existence of water or alcohol. In the formulae, R is methyl group or ethyl group, and X is hydroxy group or halide. The cyclization of the compound of the formula(2) is achieved by reaction with hydride or alkoxide at -30-50 deg.C for 1-15 hours.
Abstract translation: 目的：提供制备奥拉西坦的方法以制备高纯度奥拉西坦产物。 奥拉西坦改善脑功能和对痴呆的治疗效果。 构成：在制备式（1）的奥拉西坦的方法中，式（2）的三酰胺化合物首先通过使式（4）的有机溶剂化合物与式（2）的有机溶剂化合物 5）。 式（3）的化合物通过对式（2）的化合物依次进行环化，脱羧和还原来制备。 式（3）的化合物在水或醇存在下与氨反应。 式中，R为甲基或乙基，X为羟基或卤素。 式（2）化合物的环化通过在-30-50℃下与氢化物或醇盐反应1-15小时来实现。
-
Patent Agency Ranking
公开(公告)号：KR1020020003786A
公开(公告)日：2002-01-15
申请号：KR1020000038153
申请日：2000-07-05
Applicant: 한국화학연구원
IPC: C07D207/22
Abstract: PURPOSE: Provided is a method for preparing 3-methoxyimino-4-aminomethylpyrrolidine derivatives, which are used as a useful substituent for the position No.7 of quinolone antibiotics, from 1-benzyl-3-oxo-4-ethoxycarbo0nylpyrrolidine. CONSTITUTION: The method comprises the steps of: reacting a compound of the formula(2) with oxoamine compound or its salt to prepare a compound of the formula(3); reducing a compound of the formula(3) to prepare a compound of the formula(4); hydrogenating and amine-protecting the compound of the formula(4) to prepare a compound of the formula(5); sulfonating the compound of the formula(5) to prepare a compound of the formula(6); aminating or azidonating the compound of the formula(6) to prepare a compound of the formula(8a) or a compound of the formula(7) respectively; hydrogenating the compound of the formula(7) to prepare a compound of the formula(8a) or reacting the compound of the formula(6) with amide to prepare a compound of the formula(8b); and reacting the compound of the formula(8a) or (8b) with acid to deprotect amine.
Abstract translation: 目的：提供3-甲氧基亚氨基-4-氨基甲基吡咯烷衍生物作为喹诺酮类抗生素的第7位的有用取代基，由1-苄基-3-氧代-4-乙氧基羰基吡咯烷制备的方法。 方法：该方法包括以下步骤：使式（2）的化合物与氧代胺化合物或其盐反应以制备式（3）的化合物; 还原式（3）的化合物以制备式（4）的化合物; 氢化和胺保护式（4）化合物以制备式（5）化合物; 磺化式（5）化合物以制备式（6）化合物; 胺化或叠氮化式（6）化合物以分别制备式（8a）化合物或式（7）化合物; 氢化式（7）的化合物以制备式（8a）的化合物或使式（6）的化合物与酰胺反应以制备式（8b）的化合物; 并使式（8a）或（8b）的化合物与酸反应以使胺脱保护。
-
公开(公告)号：KR100245983B1
公开(公告)日：2000-08-01
申请号：KR1019970071789
申请日：1997-12-22
Applicant: 한국화학연구원
IPC: C07D471/04
Abstract: 본 발명은 하기 일반식(I)의 신규한 퀴놀론카르복실산 유도체 및 그의 약제학적으로 허용되는 염, 그의 제조방법 및 이를 활성 성분으로 함유하는 항균 조성물에 관한 것으로, 일반식(I)의 화합물은 항균력이 우수하고, 광범위한 항균 스펙트럼을 가지므로 항균제로 유용하다.
(상기식에서, X, R
1 , R
2 , R
3 , R
4 , R
5 및 R
6 은명세서중에서 정의한 바와 같다).-
公开(公告)号：KR100245982B1
公开(公告)日：2000-08-01
申请号：KR1019970071788
申请日：1997-12-22
Applicant: 한국화학연구원
IPC: C07D471/04
Abstract: 본 발명은 하기 일반식(I)의 신규한 퀴놀론카르복실산 유도체 및 그의 약제학적으로 허용되는 염, 그의 제조방법 및 이를 활성 성분으로 함유하는 항균 조성물에 관한 것으로, 일반식(I)의 화합물은 항균력이 우수하고, 광범위한 항균 스펙트럼을 가지므로 항균제로 유용하다.
(상기식에서, R
1 , R
2 , R
3 , R
4 및 X는 명세서중에서 정의한 바와 같다).-
公开(公告)号：KR1020000002479A
公开(公告)日：2000-01-15
申请号：KR1019980023260
申请日：1998-06-20
Applicant: 한국화학연구원
IPC: C07C215/00
Abstract: PURPOSE: Title derivatives is prepared from 5-amino-1,3-dimethyl- benzene. CONSTITUTION: 5-Amino-1,3-dimethylbenzene and chlorine iodide are reacted to give compound 3 having iodine group in 2,4- and 6-position. Compound 3 and organic acid chloride or organic acid anhydride and a base are reacted to give compound 4 substituted amino group into amido group, followed by oxidation in the presence of oxidizing agent to give compound 5. Compound 5 is halogenated or esterified to give compound 6, followed by the reaction with organic acid halide or organic acid anhydride and a base to give the title compound(I; R1 and R2 are independently H, C1-5 alkyl and C1-5 acyl, R3 and R4 are independently hydroxy, halogen, C1-5 alkoxy, benzyloxy, C1-5 alkoxycarbonyloxy, benzyloxycarbonyloxy or acetoxy).
Abstract translation: 目的：标题衍生物由5-氨基-1,3-二甲基苯制备。 构成：使5-氨基-1,3-二甲基苯和氯化碘反应，得到2,4-和6-位碘基的化合物3。 使化合物3和有机酰氯或有机酸酐和碱反应，得到化合物4取代的氨基成酰氨基，然后在氧化剂存在下进行氧化，得到化合物5.化合物5被卤化或酯化，得到化合物6 ，然后与有机酰卤或有机酸酐和碱反应，得到标题化合物（I; R 1和R 2独立地为H，C 1-5烷基和C 1-5酰基，R 3和R 4独立地是羟基，卤素， C 1-5烷氧基，苄氧基，C 1-5烷氧基羰基氧基，苄氧羰基氧基或乙酰氧基）。
-
公开(公告)号：KR1019990079064A
公开(公告)日：1999-11-05
申请号：KR1019980011452
申请日：1998-04-01
Applicant: 한국화학연구원
IPC: C07D487/10
Abstract: 본 발명은 콜레스테롤의 생합성에 관여하는 효소들 중, 특히 HMG-Co A 환원효소의 작용을 저해하는, 하기 일반식(I)의 스피로히단토인 유도체에 관한 것으로, 본 발명에 따라 제조된 히단토인 유도체는 콜레스테롤 합성효소 저해효과가 우수하여 혈중 지질농도를 저하시키는데 유리하다:
상기 식에서,
R
1 은 수소, C
1-4 알킬 또는 C
3-4 사이클로알킬이고;
R
2 은 수소, 할로겐 또는 니트로기이고;
A는 탄소 또는 질소이고;
m은 0 또는 1이고;
n은 1 또는 2이다.
-
-
-
-
-
-
-
-
-
Search Results
86
records
(took 0.029 seconds)
