环丙基苯置于溴,Potassium Acetate体系中,用 溶剂黄146 用作溶剂,化学反应生成4-溴环丙基苯 参考文献:碳离子的单电子还原.第12部分.对环丙基对苯并trop离子的稳定性及其与铬(II)离子的还原性的构象作用 标题:碳离子的单电子还原.第12部分.对环丙基对苯并trop离子的稳定性及其与铬(II)离子的还原性的构象作用 摘要:已经合成了具有和不具有侧翼甲基的一系列对-环丙基苯基tropyliumium离子以及作为参考化合物的各种甲基取代的苯基tropyliumium离子.通过1 H NMR光谱,P K R +测量以及铬(II)离子对单电子还原的速率测量,研究了对环丙基对阳离子稳定性的构象效应.检查1 H NMR光谱和这些阳离子的p K R +值表明,由于电荷离域到对位体而产生的稳定作用-环丙基随着侧翼甲基的引入而减少.当绘制铬(II)离子还原的log K 2与未取代的m-和p-甲基-,M,M-二甲基-和m-和p-甲基-的取代基常数σ +的总和时,观测到线性自由能关系.P-环丙基-Phenyltropylium离子,但登录ķ 2为p具有一个或两个侧翼甲基的β-环丙基取代的阳离子大大偏离线性相关线,反映出由于环丙基的构象变化而导致的稳定性损失. Doi:10.1039/p29790000262
专利号:US-2025092004-A1 优先权日:2022-01-14 标题:Method for producing intermediate useful for synethesis of sglt inhibitor 发明人:YOON HEE KYOON; YOON YOUN JUNG 权利人:DAEWOONG PHARMACEUTICAL CO LTD 摘要:The present invention relates to a method for producing an intermediate useful for the synthesis of an SGLT inhibitor. According to the present invention, a compound of Chemical Formula 9, which is an important intermediate for a compound of Chemical Formula 1 as an SGTL inhibitor, may be obtained with high yield and high quality. A method for producing the SGLT inhibitor according to the present invention enables production without special facilities such as an ozone generator and thus is also much more economical.
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:TW-202340162-A 优先权日:2022-01-14 标 题 :A method of preparing intermediates useful for the synthesis of sglt inhibitors
专利号:US-10889574-B2 优先权日:2016-06-17 标 题 :Method for producing diphenylmethane derivative 发明人:YOON HEE-KYOON; PARK SE-HWAN; YOON JI-SUNG; CHOI SOONGYU; SEO HEE JEONG; PARK EUN-JUNG; KONG YOUNGGYU; SONG KWANG-SEOP; KIM MIN JU; PARK SO OK 权利人:DAE WOONG PHARMA; GREEN CROSS CORP 摘要:The present invention relates to an improved method for producing a diphenylmethane derivative which is effective as a sodium-dependent glucose cotransporter (SGLT) inhibitor, the method being carried out by means of a convergent synthesis method in which each major group is separately synthesized and then coupled. As such, in comparison to a linear synthesis method disclosed in existing documents, the synthesis pathway is compact and yield can be increased, and risk factors inherent in the linear synthesis pathway can be reduced. Furthermore, the crystal form of the compound produced according to the method has superb physicochemical characteristics, and thus can be effectively utilized in fields such as pharmaceutical manufacturing.
专利号:WO-2023057548-A1 优先权日:2021-10-07 标题:Ccr6 receptor modulators 发明人:AISSAOUI HAMED; ALLEMANN OLIVER; CAROFF EVA; MEYER EMMANUEL; RICHARD-BILDSTEIN SYLVIA 权利人:IDORSIA PHARMACEUTICALS LTD 摘要:The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the prevention or treatment of e.g. inflammatory/autoimmune diseases/disorders and cancer.
专利号:US-10238631-B2 优先权日:2014-06-07 标 题 :Sesquiterpene derivatives and their use in inflammation or cancer treatment 发明人:SHYUR LIE-FEN; LEE KUO-HSIUNG; NAKAGAWA-GOTO KYOKO; FENG JIA-HUA; CHEN JO-YU; LEE WAI-LENG; CHENG YU-TING; HUANG JING-YING 权利人:ACADEMIA SINICA 摘要:A new class of sesquiterpene derivative useful for treating cancerous and inflammatory diseases are disclosed. These deoxyelephantopin derivatives are effective in suppressing proliferation, migration, mobility, invasion, growth, and/or metastasis of cancer cells in a patient, or useful for enhancing an anti-proliferative effect of another anti-cancer drug on cancer cells when treating a patient, or for sensitizing and/or enhancing an anti-cancer effect of a gluthathione synthesis blocker on inhibition of triple negative breast cancer cell activity, or for treatment and/or prophylaxis of lipopolysaccharide-stimulated inflammatory response in a patient, or for all of the above. Also disclosed are methods of preparing the deoxyelephantopin derivatives.