在 三乙基硅烷,三氟化硼乙醚体系中,用 二氯甲烷 用作溶剂,化学反应 12.0H,以0.5 G的收率获得(2S,3R,4R,5S,6R)-2-(4-氯-3-(4-乙氧基苄基)苯基)-6-(甲基硫代)四氢-2H-吡喃-3,4,5-三醇 参考文献: Process For The Preparation Of Sotagliflozin[fr] Procédé Pour La Préparation De Sotagliflozine 标题: Process For The Preparation Of Sotagliflozin[fr] Procédé Pour La Préparation De Sotagliflozine 摘要:Sotagliflozin可能使用此处披露的方案和中间体制备.Sotagliflozin可能被纳入药物剂型中,用于治疗糖尿病.
专利号:US-12358903-B2 优先权日:2016-06-13 标题 :FXR (NR1H4) modulating compounds 发明人:BLOMGREN PETER A; CURRIE KEVIN S; FARAND JULIE; GEGE CHRISTIAN; KROPF JEFFREY E; XU JIANJUN 权利人:GILEAD SCIENCES INC 摘要:The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
专利号:US-11565990-B2 优先权日:2020-12-04 标 题:Preparation of 4-bromo-2-(4′-ethoxyphenyl)-1-chlorobenzene 发明人:HU LIN; XU TAO; QIU XIAOLONG; LI XIAOYUE; ZUO ZHIWEI; LIU WENBO; CHU LINGLING; YUAN XIMENG; ZOU PING 权利人:WISDOM PHARMACEUTICAL CO LTD 摘要:A more environmentally friendly synthesis method of 4-bromo-2-(4′-ethoxyphenyl)-1-chlorobenzene with simplified steps provides a more effective synthetic strategy for producing key intermediates of SGLT-2 inhibitors such as dapagliflozin, sotagliflozin, and ertugliflozin. In the presence of trifluoroacetic anhydride, 5-bromo-2-chlorobenzoic acid and phenetole are selected to complete a direct acylation reaction under the catalysis of boron trifluoride diethyl etherate, and triethylsilane is added thereinto without treatment for one-pot reaction to obtain a target compound 4-bromo-2-(4′-ethoxyphenyl)-1-chlorobenzene.
专利号:US-11739065-B2 优先权日:2016-06-13 标题 :FXR (NR1H4) modulating compounds 发明人:BLOMGREN PETER A; CURRIE KEVIN S; GEGE CHRISTIAN; KROPF JEFFREY E; XU JIANJUN 权利人:GILEAD SCIENCES INC 摘要:The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
专利号:CN-110818722-B 优先权日:2018-08-14 标 题:Three compounds, their preparation methods and their application in the synthesis of soxagliflozin
专利号:US-2020255394-A1 优先权日:2018-09-26 标题 :Crystalline solid forms of n-(1-((2-(dimethylamino)ethyl)amino)-2-methyl-1-oxopropan-2-yl)-4-(4-(2-methyl-5-((2s,3r,4r,5s,6r)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2h-pyran-2-yl)benzyl)phenyl)butanamide and methods of their synthesis
专利号:CA-3113037-A1 优先权日:2018-09-26 标 题 :Crystalline forms of n-(1-((2-(dimethylamino)ethyl)amino)-2-methyl-1-oopropan-2-yl)-4-(4-(2-methyl-5-(2s,3r,4r,5s,6r)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2h-pyran-2-yl)benzyl)phenl)butanamide and methods of their synthesis