葡萄糖酸内酯置于n-甲基吗啉,三甲基氯硅烷体系中,用 四氢呋喃 用作溶剂,化学反应 20.0H,反应生成2,3,4,6-四-O-三甲基硅基-D-葡萄糖酸内酯 参考文献:[de] Glucopyranosyl-Substituierte Benzol-Derivate,Diese Verbindungen Enthaltende Arzneimittel,Deren Verwendung Und Verfahren Zu Ihrer Herstellung Glucopyranosyl-Substituted Benzol Derivatives,Drugs Containing Said Compounds,The Use Thereof And Method For The Production Thereof[fr] Derives Du Benzol Substitues Par Un Glucopyranosyle,,Medicaments Renfermant Ces Composes,Leur Utilisation Et Leur Procede De Production 标题:[de] Glucopyranosyl-Substituierte Benzol-Derivate,Diese Verbindungen Enthaltende Arzneimittel,Deren Verwendung Und Verfahren Zu Ihrer Herstellung Glucopyranosyl-Substituted Benzol Derivatives,Drugs Containing Said Compounds,The Use Thereof And Method For The Production Thereof[fr] Derives Du Benzol Substitues Par Un Glucopyranosyle,,Medicaments Renfermant Ces Composes,Leur Utilisation Et Leur Procede De Production 摘要:通用式(I)的葡萄糖吡喃基取代苯衍生物,其中残基r1至r6以及r7A,R7B,R7C如权利要求1所定义,包括它们的互变异构体,立体异构体,混合物和盐.这些化合物适用于治疗代谢疾病.
专利号:WO-2017063617-A1 优先权日:2015-10-13 标 题 :Preparation of intermediates for the synthesis of canagliflozin and dapagliflozin 发明人:ZEZULA JOSEF; BABIAK PETR; HAJDUCH JAN 权利人:ZENTIVA KS 摘要:The present invention relates to a preparation method of the intermediates of structures la (for the synthesis of canagliflozin) and 1b (for the synthesis of dapagliflozin), where in structure la X is methyl and Ar represents 2-(5-(4-fluorophenyl)-thienyl) and in structure 1b X is chlorine and Ar represents 4-ethoxyphenyl.
专利号:US-2007293690-A1 优先权日:2004-07-08 标题:Process for Production of Azulene Derivatives and Intermediates for the Synthesis of the Same 发明人:TOMIYAMA HIROSHI; YOKOTA MASAYUKI; NODA ATSUSHI; KOBAYASHI YOSHINORI; OGASAWARA JUNKO; HAYASHI YASUMASA; INAKOSHI MASATOSHI; NAKAMURA HIROFUMI; KOIDE TOKUO; SAKAMOTO KENICHIRO; YAMASHITA YOHEI; MIYAFUJI AKIO; SUZUKI TAKAYUKI; KAWANO NORIYUKI; MIYATA JUNJI; IMAMURA MASAKAZU; SUGANE TAKASHI 权利人:TOMIYAMA HIROSHI; YOKOTA MASAYUKI; NODA ATSUSHI; KOBAYASHI YOSHINORI; OGASAWARA JUNKO; HAYASHI YASUMASA; INAKOSHI MASATOSHI; NAKAMURA HIROFUMI; KOIDE TOKUO; SAKAMOTO KENICHIRO; YAMASHITA YOHEI; MIYAFUJI AKIO; SUZUKI TAKAYUKI; KAWANO NORIYUKI; MIYATA JUNJI; IMAMURA MASAKAZU; SUGANE TAKASHI 摘要:A process for producing an azulene derivative useful as a Na + -glucose cotransporter inhibitor, which is high in yield, is simple in operation, is low in cost, is suited for environmental protection, and is advantageous industrially, the process being characterized by reducing and deprotecting at least one compound selected from penta-acyl compounds and tetra-acyl compounds or salts thereof to obtain a C-glycoside compound; and a useful intermediate for synthesis of such an azulene derivative, obtained in the course of the above process.
专利号:US-9018249-B2 优先权日:2011-09-13 标题 :SGLT inhibitors 发明人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR 权利人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR; PANACEA BIOTEC LTD 摘要:The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula I and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).
专利号:US-2014228303-A1 优先权日:2011-06-13 标题 :Novel sglt inhibitors 发明人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR 权利人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR; PANACEA BIOTEC LTD 摘要:The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula I and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).
专利号:MX-2007000209-A 优先权日:2004-07-08 标题 :PROCESS FOR THE PRODUCTION OF AZULEN DERIVATIVES AND INTERMEDIARIES FOR THE SYNTHESIS OF THE SAME.
专利号:EP-1783122-A1 优先权日:2004-07-08 标 题 :Process for production of azulene derivatives and intermediates for the synthesis of the same