CAS: 163706-06-7; (Dichloro((((((2R,3S,4R,5R)-3,4-Dihydroxy-5-(6-((2-(Methylthio)Ethyl)Amino)-2-((3,3,3-Trifluoropropyl)Thio)-9H-Purin-9-yl)Tetrahydrofuran-2-yl)Methoxy)(Hydroxy)Phosphoryl)Oxy)(Hydroxy)Phosphoryl)Methyl)Phosphonic Acid

上下游产品

坎格瑞洛中间体3 N-[2-(Methylthio)Ethyl]-2-[(3,3,3-Trifluoropropyl)Thio]-5'-Adenylic Acid 847460-53-1
N6-(2-甲硫基乙基) -2-(3,3,3-三氟丙硫基)腺苷 6-N-[2-(Methylthio)Ethyl]-2-[(3,3,3-Trifluoropropyl)Thio]Adenosine 163706-58-9
坎格雷洛杂质 2-[(3,3,3-Trifluoropropyl)Thio]Adenosine 163706-51-2
2-硫代腺苷酸 2-Thioadenosine 43157-50-2

坎格雷洛杂质置于吡啶,甲醇,Sodium Hydroxide,三正丁胺,磷酸三乙酯,Sodium Acetate,Sodium Hydride,碳酸氢钠,N,N'-羰基二咪唑,三氯氧磷体系中,用 甲醇,N,N-二甲基甲酰胺 用作溶剂,化学反应 37.25H,反应生成坎格雷洛
参考文献:Antagonists Of The Platelet P2T Receptor: A Novel Approach To Antithrombotic Therapy
标题:Antagonists Of The Platelet P2T Receptor: A Novel Approach To Antithrombotic Therapy
摘要:The Platelet P(2T) Receptor Plays A Major Role In Platelet Aggregation,And Its Antagonists Are Predicted To Have Significant Therapeutic Potential As Antithrombotic Agents. We Have Explored Analogues Of Adenosine Triphosphate (Atp),Which Is A Weak,Nonselective But Competitive P(2T) Receptor Antagonist. Modification Of The Polyphosphate Side Chain To Prevent Breakdown To The Agonist Adenosine Diphosphate (Adp) And Substitution Of The Adenine Moiety To Enhance Affinity And Selectivity For The P(2T) Receptor Led To The Identification Of 10E (Ar-C67085Mx),Having An Ic(50) Of 2.5 Nm Against Adp-Induced Aggregation Of Human Platelets. Compound 10E Was The First Very Potent Antagonist Of The P(2T) Receptor,With A Selectivity For That Subtype Of The P2 Receptor Family Of >1000-Fold. Further Modification Of The Structure Produced Compound 101 (Ar-C69931Mx) Having An Ic(50) Of 0.4 Nm. In Vivo,At Maximally Effective Antithrombotic Doses,There Is Little Prolongation Of Bleeding Time (1.4-Fold),Which Is In Marked Contrast To The 5-6-Fold Found With Gpiib/liia Antagonists.
Doi:10.1021/jm981072S

专利信息

专利号:US-8017776-B2
优先权日:2003-07-15
标题 :Methods for synthesis of acyloxyalkyl compounds
发明人：BHAT LAXMINARAYAN; GALLOP MARK A
权利人:XENOPORT INC
摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

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.

专利号:US-8143437-B2
优先权日:2002-02-19
标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
发明人：GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X
权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC
摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

专利号:US-2010317848-A1
优先权日:2006-12-31
标题:Process for the synthesis of derivatives of 3-amino-tetrahydrofuran-3-carboxylic acid and use thereof as medicaments

专利号:EP-4499223-A1
优先权日:2022-03-31
标 题 :Synthesis of morphinans with reduced herg activity and mop binding

专利号:US-2005070715-A1
优先权日:2003-07-15
标 题:Methods for synthesis of acyloxyalkyl compounds