CAS: 842133-18-0; (2S,3R,4R,5S,6R)-2-(3-((5-(4-Fluorophenyl)Thiophen-2-yl)Methyl)-4-Methylphenyl)-6-(Hydroxymethyl)Tetrahydro-2H-Pyran-3,4,5-Triol

上下游产品

CAS号1283129-18-9 (2S,3S,4R,5R,6R... | CAS号866607-35-4 坎格列净四乙酸酯 | CAS号1030825-21-8 甲基 1-C-[3-[[5-(... | CAS号492-62-6 α-D-葡萄糖 | CAS号1213234-53-7 1,2,3,4,6-penta... | CAS号898566-17-1 2-(4-氟苯基)-5-((5... | CAS号81058-27-7 2,3,4,6-O-四特戊酰基... | CAS号1283129-24-7 bis(3-((5-(4-fl... | CAS号498-07-7 1,6-脱水-β-D-葡萄糖

A-无水葡萄糖酯置于吡啶,4-二甲氨基吡啶,正丁基锂,水,异丙基氯化镁,Lithium Chloride,Potassium Hydroxide,Zinc Dibromide体系中,用 四氢呋喃,甲醇,正己烷,二氯甲烷 作为反应溶剂,化学反应 63.58H,反应生成 卡格列净
参考文献:卤代新戊酰基吡喃葡萄糖及其用于sglt2抑 制剂的制备方法
标题:卤代新戊酰基吡喃葡萄糖及其用于sglt2抑 制剂的制备方法
摘要:本发明属于药物合成技术领域,本发明涉及用于制备对存在于肠或肾内的钠依赖性葡萄糖转运蛋白(Sglt)具有抑制活性的化合物(包括坎格列净,达格列净,恩格列净,伊格列净)的新方法.本发明公开了1,2,3,4,6‐五‐o‐卤代新戊酰基吡喃葡萄糖,其结构通式为式ⅰ,本发明还同时公开了2,3,4,6‐四‐o‐卤代新戊酰基‐α‐d‐卤代吡喃葡萄糖(简称卤代葡萄糖),其结构通式为式ⅲ;本发明还同时公开了一种sglt2抑制剂的制备方法.采用本发明的方法制备sglt2抑制剂,具有纯度高,收率较高,操作简便,适合工业化生产等技术优势.

专利信息

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-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:EP-2918579-A1
优先权日:2014-03-14
标题 :Synthesis of 2-arylmethyl-5-aryl-thiophene
权利人:LEK PHARMACEUTICALS
摘要:The present invention provides a new synthetic process for the production of 2-arylmethyl-5-aryl-thiophene, an intermediate in the synthesis of C-aryl glycosides.

专利号:US-11485721-B2
优先权日:2017-11-21
标 题:Method for the metal-free preparation of a biaryl by a photosplicing reaction and their uses
发明人：KLOSS FLORIAN; NEUWIRTH TONI; HAENSCH VEIT; HERTWECK CHRISTIAN
权利人:LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST HKI; LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST
摘要:The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar—Ar′ by photochemically reacting a precursor compound of formula (II): Ar—L—Ar′ to form a biaryl compound of general formula: Ar—L—Ar′(II)→Ar—Ar′ (I) wherein Ar and Ar′, independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5-20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group —X—Y—Z— as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.

专利号:US-2017247359-A1
优先权日:2014-09-05
标题 :Process for the preparation of canagliflozin
发明人：VELLANKI SIVA RAM PRASAD; BALUSU RAJA BABU; PILLI RAMAKRISHNA; JAWAJI RAJESWARA ROA; ANNADASU ANKAMA NAYUDU
权利人:MYLAN LABORATORIES LTD
摘要:A process for the preparation of canagliflozin. The process may be effectively implemented on an industrial scale. Several compounds useful as intermediates for the synthesis of canagliflozin (Formula 4, Formula 4a, Formula 4b and Formula 5) are also disclosed. The process involves the reduction of the compound of formula 3 in the presence of a metal hydride and an organic solvent to obtain the compound of formula 4, converting this into a compound of formula 5 which in turn is converted into canagliflozin.

专利号:US-2025223262-A1
优先权日:2022-03-31
标 题 :Synthesis of morphinans with reduced herg activity and mop binding
发明人：LAMMERT ECKHARD; SCHOLZ OKKA; OTTER SILKE; HEREBIAN DIRAN; HOFFMANN TORSTEN; SANZ MIGUEL ANGEL; KRAMP LAURENZ; LEVY LAURA MARIANA; HRISTEVA STANIMIRA
权利人:HEINRICH HEINE UNIV DUESSELDORF; DEUTSCHE DIABETES FORSCHUNGSGESELLSCHAFT E V; TAROS CHEMICALS GMBH & CO KG
摘要:The invention relates to morphinan-derivatives, processes for their preparation, medicaments containing them and the use of these morphinan-derivatives for the preparation of medicaments.