CAS: 461432-25-7; (2R,3R,4R,5S,6S)-2-(Acetoxymethyl)-6-(4-Chloro-3-(4-Ethoxybenzyl)Phenyl)Tetrahydro-2H-Pyran-3,4,5-Triyl Triacetate

上下游产品

达格列嗪 Dapagliflozin 461432-26-8
Dapagliflozin 1118566-45-2
甲基 1-C-[4-氯-3-[(4-乙氧基苯基)甲基]苯基]-D-吡喃葡萄糖苷 (3R,4S,5S,6R)-2-(4-Chloro-3-(4-Ethoxybenzyl)Phenyl)-6-(Hydroxymethyl)-2-Methoxytetrahydro-2H-Pyran-3,4,5-Triol 461432-24-6
(2S,3R,4S,5S,6R)-2-(4-氯-3-(4-乙氧基苄基)苯基)-6-(羟甲基)-2-甲氧基四氢-2H-吡喃-3,4,5-三醇 (2S,3R,4S,5S,6R)-2-(4-Chloro-3-(4-Ethoxybenzyl)Phenyl)-6-(Hydroxymethyl)-2-Methoxytetrahydro-2H-Pyran-3,4,5-Triol 714269-57-5
(3R,4S,5R,6R)-2-(4-氯-3-(4-乙氧基苄基)苯基)-3,4,5-三((三甲基甲硅烷基)氧基)-6-(((三甲基甲硅烷基)氧基)甲基)四氢-2H-吡喃-2-醇 (3R,4S,5R,6R)-2-(4-Chloro-3-(4-Ethoxybenzyl)Phenyl)-3,4,5-Tris((Trimethylsilyl)Oxy)-6-(((Trimethylsilyl)Oxy)Methyl)Tetrahydro-2H-Pyran-2-Ol 960494-15-9

葡萄糖酸内酯置于n-甲基吗啉,吡啶,三乙基硅烷,4-二甲氨基吡啶,正丁基锂,甲烷磺酸,三氟化硼乙醚体系中,用 四氢呋喃,正己烷,二氯甲烷,甲苯,乙腈 作为反应溶剂,化学反应 7.5H,反应生成 (2R,3R,4R,5S,6S)-2-(乙酰氧基甲基)-6-(4-氯-3-(4-乙氧基苄基)苯基)四氢-2H-吡喃-3,4,5-三yl 三乙酸酯
参考文献:达格列净释放一氧化氮的潜在抗糖尿病和抗血栓形成剂的设计,合成和生物学评价
标题:达格列净释放一氧化氮的潜在抗糖尿病和抗血栓形成剂的设计,合成和生物学评价
摘要:心血管并发症在2型糖尿病(t2Dm)中非常普遍,甚至在t2Dm的早期阶段或强化血糖控制状态下也是如此.因此,迫切需要在t2Dm中干预心血管并发症.本文中,设计了no供体和sglt2抑制剂的新杂种以获得抗高血糖和抗血栓形成的双重作用.如所预期的,优选的杂种2表现出中等的sglt2抑制作用和抗血小板聚集活性,并且在no清除剂的存在下也证实了其由no介导的抗血小板作用.此外,化合物2在小鼠的口服葡萄糖耐量试验中发现了显着的降血糖作用和尿葡萄糖排泄.潜在的多功能复合物(例如化合物2)有望作为干预t2Dm中心血管并发症的潜在候选药物.
DOI:10.1016/j.Bmc.2018.06.017

专利信息

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-8791077-B2
优先权日:2008-05-22
标 题:Method for treating hyperuricemia employing an SGLT2 inhibitor and composition containing same
发明人：LESLIE BRUCE ROBERT
权利人:LESLIE BRUCE ROBERT; ASTRAZENECA AB
摘要:Methods are provided for treating hyperuricemia, employing an SGLT2 inhibitor alone, or in combination with a supply of carbohydrate, and/or in combination with an inhibitor of uric acid synthesis. Additionally, pharmaceutical compositions comprising an SGLT2 inhibitor with a supply of carbohydrate or an inhibitor of uric acid synthesis or a supply of carbohydrate and an inhibitor of uric acid synthesis are provided in the instant invention and are provided for use in the inventive methods.