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Patent Agency Ranking1.发明申请SYNTHESIS OF N-GLYCOSYLATED COMPOUNDS WITH THE USE OF A MILD, IODINE-CATALYZED REACTION 审中-公开N-甲酰化合物的合成与使用微量的碘化反应
公开(公告)号：WO1994007900A1
公开(公告)日：1994-04-14
申请号：PCT/US1993009036
申请日：1993-09-23
IPC: C07H05/04
Abstract: The invention concerns N-glycosylated derivatives of nitrogen nucleophile compounds. The invention also concerns a mild, cost effective, stereoselective, regioselective, and generally applicable method for the preparation of N-glycosides by N-glycosylation of azide and amide nucleophile compounds. The method employs iodine in a catalytic amount that uniquely does not pose an environmental hazard. The invention provides efficient access to key intermediates for the synthesis inter alia of analogs of AZT and DDI and for the synthesis of conventional N-nucleoside antibiotic drugs and their novel N-glycosylated analogs.
Abstract translation: 本发明涉及氮亲核化合物的N-糖基化衍生物。 本发明还涉及通过叠氮化物和酰胺亲核化合物的N-糖基化制备N-糖苷的温和，成本有效的立体选择性，区域选择性和通常适用的方法。 该方法采用催化量的碘，其独特地不会造成环境危害。 本发明提供了用于合成特别是AZT和DDI的类似物以及用于合成常规N-核苷抗生素药物及其新型N-糖基化类似物的关键中间体的有效接触。
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公开(公告)号：WO1995032956A1
公开(公告)日：1995-12-07
申请号：PCT/US1995006715
申请日：1995-05-26
Inventor： THE BOARD OF REGENTS acting for and on behalf of THE UNIVERSITY OF MICHIGAN , KOREEDA, Masato , SHULL, Brian, K. , YANG, Wu
IPC: C07D327/06
CPC classification number: C07H15/26
Abstract: Novel water-soluble mono and disaccharides of 1,2-dithiins, as well as methods for their synthesis and the synthesis of 3,6-bis(hydroxymethyl)-1,2-dithiin, are provided. The water-soluble compounds have useful medicinal applications, e.g., as an antifungal agent or antibacterial agent in a pharmaceutically acceptable carrier.
Abstract translation: 提供了1,2-二噻吩的新型水溶性单二糖和二糖，以及它们的合成方法和3,6-双（羟甲基）-1,2-二噻吩的合成。 水溶性化合物具有有用的医学应用，例如在药学上可接受的载体中作为抗真菌剂或抗菌剂。
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3.发明申请SYNTHESIS OF C-GLYCOSYLATED COMPOUNDS WITH THE USE OF A MILD, IODINE-CATALYZED REACTION 审中-公开使用C-GLYCOSYLATED化合物与微量元素催化反应的合成
公开(公告)号：WO1994007899A1
公开(公告)日：1994-04-14
申请号：PCT/US1993009037
申请日：1993-09-23
Inventor： THE BOARD OF REGENTS acting for and on behalf of ... , KOREEDA, Masato , HOUSTON, Todd, A.
IPC: C07H01/00
CPC classification number: C07D307/32 , C07D309/30
Abstract: The invention concerns C-glycosylated derivatives of soft carbon nucleophile compounds, particularly compounds which contain acid-labile structural units. The invention further concerns a mild, cost-effective, non-hazardous and stereoselective method of general application employing a glycal as a glycosylating agent and iodine as a catalyst for the preparation of C-glycosylated soft carbon nucleophile compounds.
Abstract translation: 本发明涉及软碳亲核试剂化合物的C-糖基化衍生物，特别是含酸不稳定结构单元的化合物。 本发明还涉及使用甘氨酸作为糖基化剂和碘作为制备C-糖基化的软碳亲核化合物的催化剂的一般应用的温和的，具有成本效益的非危险和立体选择性方法。
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4.发明公开WATER-SOLUBLE GLYCOSYLATED DERIVATIVES OF 1,2-DITHIIN COMPOUNDS 失效1,2- DITHIINVERBINDUNGEN水溶性糖基化的衍生物
公开(公告)号：EP0765316A1
公开(公告)日：1997-04-02
申请号：EP95921450.0
申请日：1995-05-26
Inventor： KOREEDA, Masato , SHULL, Brian, K. , YANG, Wu
IPC: C07H15
CPC classification number: C07H15/26
Abstract: Novel water-soluble mono and disaccharides of 1,2-dithiins, as well as methods for their synthesis and the synthesis of 3,6-bis(hydroxymethyl)-1,2-dithiin, are provided. The water-soluble compounds have useful medicinal applications, e.g., as an antifungal agent or antibacterial agent in a pharmaceutically acceptable carrier.
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5.发明授权WATER-SOLUBLE GLYCOSYLATED DERIVATIVES OF 1,2-DITHIIN COMPOUNDS 失效1,2- DITHIINVERBINDUNGEN水溶性糖基化的衍生物
公开(公告)号：EP0765316B1
公开(公告)日：2002-07-31
申请号：EP95921450.3
申请日：1995-05-26
Inventor： KOREEDA, Masato , SHULL, Brian, K. , YANG, Wu
IPC: C07H15/26 , C07D339/08
CPC classification number: C07H15/26
Abstract: Novel water-soluble mono and disaccharides of 1,2-dithiins, as well as methods for their synthesis and the synthesis of 3,6-bis(hydroxymethyl)-1,2-dithiin, are provided. The water-soluble compounds have useful medicinal applications, e.g., as an antifungal agent or antibacterial agent in a pharmaceutically acceptable carrier.
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