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1. 发明授权

KR101057239B1 뉴클레오사이드 리보푸라노실 피리미딘의 제조 有权
公开(公告)号：KR101057239B1
公开(公告)日：2011-08-16
申请号：KR1020097008991
申请日：2007-10-05
申请人： 길리어드 파마셋 엘엘씨 , 에프. 호프만-라 로슈 아게
发明人： 악스트스티븐디. , 사르마케샵 , 비탈레저스틴 , 즈후지앙 , 로스브루스 , 라차콘다수구나 , 진큉우 , 전병권
IPC分类号： C07H19/06 , C07H5/02
CPC分类号： C07H5/02 , C07H1/00 , C07H19/06
摘要： The present process provides an improved method for the preparation of 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-hydrox-ymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one of the formula (IV) which is a potent inhibitor of Hepatitis C Virus (HCV) NS5B polymerase.

2. 发明授权

KR101024882B1 수크랄로스 정제를 위한 추출 방법 失效
标题翻译：纯化三氯蔗糖的萃取方法
公开(公告)号：KR101024882B1
公开(公告)日：2011-03-31
申请号：KR1020047014006
申请日：2003-03-06
申请人： 테이트 앤드 라일 퍼블릭 리미티드 컴파니
发明人： 캐타니스티븐제이. , 버넌니콜라스엠. , 네이디크데이비드사울 , 윌리제임스에드윈 , 미킨스키에드워드
IPC分类号： C07H1/06 , C07H5/02
CPC分类号： C07H5/02 , C07H1/06
摘要： 본 발명은 수크랄로스 정제를 위한 신규한 추출 방법에 관한 것이다. 본 발명은 또한 본 발명의 방법에 의해 생성된 수크랄로스 제제를 포함하는 조성물에 관한 것이다.

3. 发明公开

KR1020090082422A 트라이포스겐 (ＢＴＣ)에 의한 당의 염소화에 의한 수크랄로스의 제조 방법 无效
标题翻译：通过三氯乙酸（BTC）酿造糖制备蔗糖的方法
公开(公告)号：KR1020090082422A
公开(公告)日：2009-07-30
申请号：KR1020097010474
申请日：2007-10-24
申请人： 맘테크 인터내셔널 리미티드
发明人： 호,데이비드로산 , 완,정하오
IPC分类号： C07H1/00 , C07H5/02 , C13K5/00 , C13K7/00
CPC分类号： C07H1/00 , C07H5/02
摘要： In one embodiment of the invention a method to prepare sucralose-6-acylate through chlorinating sucrose-6-acylater by BTC in the process of sucralose preparation is disclosed. In this embnodiment a Vilsmeier reagent is firstly prepared belowe 0 °C by dissolving BTC in DMF or in component solvent, containing DMF, toluene, dichloroethane, chloroform and carbon tetrachloride. Consequently, sucrose-6-ester was chlorinated by Vilsmeier reagent. BTC can also be dissolved in one or several organic solvent such as toluene, dichloroethane, chloroform and carbon tetrachloride, and added to a DMF solution of sucrose-6-acylate for chlorination. Sucralose was prepared through de-esterifying the obtained sucralosed 6-ester using sodium methoxide/methanol or sodium ethoxide/ethanol.
摘要翻译：在本发明的一个实施方案中，公开了通过在三氯蔗糖制备过程中通过BTC氯化蔗糖-6-酰化物来制备三氯蔗糖-6-酰化物的方法。在此实施例中，首先通过将BTC溶解在DMF中或在含有DMF，甲苯，二氯乙烷，氯仿和四氯化碳的组分溶剂中于0℃下制备Vilsmeier试剂。因此，蔗糖-6-酯被Vilsmeier试剂氯化。 BTC也可以溶解在一种或几种有机溶剂如甲苯，二氯乙烷，氯仿和四氯化碳中，并加入蔗糖-6-酰化物的DMF溶液进行氯化。通过使用甲醇钠/甲醇或乙醇钠/乙醇使得到的三氯蔗糖6-酯脱酯化来制备三氯蔗糖。

4. 发明公开

KR1020090060460A 뉴클레오사이드 리보푸라노실 피리미딘의 제조 有权
标题翻译：核糖核苷酸嘧啶的制备
公开(公告)号：KR1020090060460A
公开(公告)日：2009-06-12
申请号：KR1020097008991
申请日：2007-10-05
申请人： 길리어드 파마셋 엘엘씨 , 에프. 호프만-라 로슈 아게
发明人： 악스트스티븐디. , 사르마케샵 , 비탈레저스틴 , 즈후지앙 , 로스브루스 , 라차콘다수구나 , 진큉우 , 전병권
IPC分类号： C07H19/06 , C07H5/02
CPC分类号： C07H5/02 , C07H1/00 , C07H19/06
摘要： The present process provides an improved method for the preparation of 4-amino-l-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydro-furan-2-yl)-lH-pyrimidin-2-one of the formula (IV) which is a potent inhibitor of Hepatitis C Virus (HCV) NS5B polymerase.
摘要翻译：本方法提供了制备4-氨基-1 - （（2R，3R，4R，5R）-3-氟-4-羟基-5-羟甲基-3-甲基 - 四氢 - 呋喃-2-基吡啶-2-基）-1H-（嘧啶-2-基）-1H-咪唑-2-酮，其是丙型肝炎病毒（HCV）NS5B聚合酶的有效抑制剂。

5. 发明公开

KR1020090007556A 염소화 시약의 제조 공정 및 염소화 당의 제조에 있어 그의용도 无效
标题翻译：生产氯仿试剂的过程及其在制备氯化糖中的应用
公开(公告)号：KR1020090007556A
公开(公告)日：2009-01-19
申请号：KR1020087022691
申请日：2007-02-28
申请人： 브이.비. 메디케어 프리베이트 엘티디.
发明人： 라트남,라케쉬 , 오로라,선디프 , 모피주딘,모하메드
IPC分类号： C07H1/00 , C07H13/02 , C07H15/00 , C07H5/02
CPC分类号： C07H1/00 , C07H5/02 , C07H13/02 , C07H15/00
摘要： Preparation of chlorinating reagent or chlorination reaction itself for use in a reaction such as production of high intensity sweetener trichlorogalactosucrose (TGS) from partially protected sucrose comprising reaction of dimethylformamide (DMF) with thionyl chloride or another sulphur containing inorganic acid chlorides including sulphuryl chloride is faced with a problem of prolific release of gaseous by-products, that at times may lead to violent explosion also. This problem is solved by innovative addition of solid powder inert to the constituents of the chlorination reaction mixture to the reaction, or by adding DMF to acid chloride solution in that order. The invention also leads to use of isolated solid Vilsmeier reagent being used for chlorination in a solvent other than DMF making it possible to avoid altogether problems arising from use of DMF which include irrecoverable loss in alkaline as well as acid conditions, interference in crystallization of TGS and the like.
摘要翻译：制备氯化试剂或氯化反应本身用于反应，例如从部分保护的蔗糖生产高强度甜味剂三氯半乳蔗糖（TGS），包括二甲基甲酰胺（DMF）与亚硫酰氯或另一种含硫的无机酰氯（包括磺酰氯）的反应存在气态副产物多产释放的问题，有时也可能导致剧烈的爆炸。通过将氯化反应混合物的成分惰性的固体粉末添加到反应中，或者通过向该酰氯溶液中依次加入DMF来解决这个问题。本发明还导致使用分离的固体维尔斯迈尔试剂用于在DMF以外的溶剂中进行氯化，使得可以避免使用DMF引起的一切问题，其包括在碱性和酸性条件下不可恢复的损失，TGS的结晶干扰等等。

6. 发明公开

KR1020080043342A 소수성 친화 크로마토그래피에 따른 염소화 당 제조방법 无效
标题翻译：基于亲水性亲和色谱法生产氯化蔗糖的方法
公开(公告)号：KR1020080043342A
公开(公告)日：2008-05-16
申请号：KR1020087005898
申请日：2006-08-29
申请人： 브이.비. 메디케어 프리베이트 엘티디.
发明人： 라트남,라케쉬 , 오로라,선디프 , 케일,산디프,바스카 , 라리,아르빈드,말리나트
IPC分类号： C07H1/06 , C07H5/02
CPC分类号： C07H1/06 , C07H5/02
摘要： This invention relates to a process for selective capture, isolation and purification of chlorinated sucrose compounds, including chlorinated sucrose, their precursors and derivatives, including trichlorogalactosucrose (TGS), directly from chlorinated reaction mixture by column chromatography on adsorbents and under conditions which result in specific and selective affinity towards one or more of chlorinated sucrose compound. The process also integrates de-esterification of chlorinated sucrose esters adsorbed on the adsorbent while they are being treated with desorbent. The process also provides a novel approach to concentration and crystallization of TGS. The chlorinated sucrose derivatives, including TGS, thus isolated are substantially free from most impurities, salts and organic solvents. The process has high recovery of more than 95% in terms of desired chlorinated sucrose derivatives including TGS.
摘要翻译：本发明涉及一种选择性捕获，分离和纯化氯化蔗糖化合物的方法，包括氯化蔗糖，其前体和衍生物，包括三氯半乳糖（TGS），直接由氯化反应混合物通过柱色谱法在吸附剂上和在导致特异性以及对一种或多种氯化蔗糖化合物的选择性亲和力。该方法还将吸附在吸附剂上的氯化蔗糖酯的脱酯化同时用解吸剂进行处理。该方法还提供了TGS的浓缩和结晶的新方法。由此分离的氯化蔗糖衍生物，包括TGS基本上不含大多数杂质，盐和有机溶剂。该方法在所需的氯代蔗糖衍生物（包括TGS）方面具有高于95％的高回收率。

7. 发明授权

KR100024981B1 4'-할로-치환 자당 유도체의 제조방법 失效
标题翻译：制备4'-卤代糖衍生物的方法
公开(公告)号：KR100024981B1
公开(公告)日：1988-02-05
申请号：KR1019820001851
申请日：1982-04-27
申请人： 테이트앤드라일퍼블릭리미티드컴퍼니
发明人： 그레함잭슨 , 마이클탈프제너 , 리아즈아메드칸 , 청관리 , 키쟈트슬탄멉티 , 지타달립파텔 , 엘너브린라드븐
IPC分类号： C07H5/02 , C07H3/04

8. 发明公开

KR870004149A 신규의 테트라클로로라피노스 및 슈크랄로스 제조에의 사용법 失效
公开(公告)号：KR870004149A
公开(公告)日：1987-05-07
申请号：KR860008778
申请日：1986-10-20
IPC分类号： A23G3/38 , A23G3/34 , C07H1/00 , C07H3/04 , C07H5/02 , C12P19/00 , C12P19/14 , C12P19/20 , C12R1/645 , C12R1/685
摘要： 내용없음

9. 发明授权

KR850000078B1 4,1',6'-트리클로로-4,1',6'-트리데옥시-갈락토슈크로오스의 제법 失效
公开(公告)号：KR850000078B1
公开(公告)日：1985-02-18
申请号：KR800004846
申请日：1980-12-19
申请人： TATE & LYLE PATENT HOLDINGS
发明人： JACSON GRAHAM , JENNER MICHAEL RALPH , WILLIAMS JOHN CLIVE , WAITE DAVID
IPC分类号： C07H5/02 , C07H5/00

10. 发明公开

KR1020170015575A （1Ｓ,4Ｒ） - 2 - 옥사 - 3 - 아자비시클로 ［2.2.1］ 헵트 - 5 - 엔의 제조 방법 无效
标题翻译： 14-2 - - 3 - 2.2.1 - 5 - 制备14-2-OXA-3-AZABYYCLO [2.2.1] HEPT-5-ENES的方法
公开(公告)号：KR1020170015575A
公开(公告)日：2017-02-08
申请号：KR1020177003043
申请日：2010-08-25
申请人： 론자 리미티드
发明人： 프란첸마누엘라 , 노티크리슈티안
IPC分类号： C07D265/34 , C07D261/08 , C07H5/02 , C07H5/00
CPC分类号： C07D265/34 , Y02P20/55 , C07D261/08 , C07H5/00 , C07H5/02
摘要： 본발명에따르면, 하기화학식의거울상이성질적으로강화된 (1S,4R) - 2 - 옥사 - 3 - 아자비시클로 [2.2.1] 헵트 - 5 - 엔:[식중, PG은아미노-보호기임] 은하기화학식의보호된 1 -- 니트로소 - β - D - 리보푸라노실할라이드:[식중, X 는불소, 염소, 브롬및 요오드로부터선택되는할로겐원자이고, PG는히드록실-보호기이고, PG는 1,2 - 디올-보호기임] 와의헤테로-디엘스-알더고리화첨가를통해시클로펜타디엔으로부터제조된다.
摘要翻译：具有下式的对映异构富集（1S，4R）-2-氧杂-3-氮杂双环[2.2.1]庚-5-烯：其中PG1是氨基保护基，是由环戊二烯通过杂 - 狄尔斯 - 阿尔德环加成与保护的 1-C-亚硝基和D-呋喃核糖基卤化物，其中X是选自氟，氯，溴和碘的卤素原子，PG2是羟基保护基，PG3是1,2-二醇保护基。

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