CAS: 376608-74-1; 2-(((3Ar,4S,6R,6As)-6-((5-Amino-6-Chloro-2-(Propylthio)Pyrimidin-4-yl)Amino)-2,2-Dimethyltetrahydro-3Ah-Cyclopenta[d][1,3]Dioxol-4-yl)Oxy)Ethanol

欧盟法规

[REACH注册ECHA物质

甲基-2,3-O-异亚丙基-D-呋喃核糖苷置于吡啶,锂硼氢,Palladium 10% On Activated Carbon,5%-Palladium/activated Carbon,氢气,Sodium Hydride,Sodium Carbonate,三乙胺,N,N-二异丙基乙胺,Sodium Iodide,锌体系中,用 四氢呋喃,1,4-二氧六环,甲醇,乙醇,N,N-二甲基甲酰胺,4-甲基-2-戊酮,甲苯,丁酮 用作溶剂,化学反应 87.5H,反应生成2-[[(3Ar,4S,6R,6As)-6-[[5-氨基-6-氯-2-(丙硫基)-4-嘧啶基]氨基]四氢-2,2-二甲基-4H-环戊烯并-1,3-二恶茂-4-基]氧基]乙醇
参考文献:Synthesis And Biological Evaluation Of Ticagrelor Derivatives As Novel Antiplatelet Agents
标题:Synthesis And Biological Evaluation Of Ticagrelor Derivatives As Novel Antiplatelet Agents
摘要:Ticagrelor (1) Is The First Reversible P2Y12 Receptor Antagonist Blocking Adenine Diphosphate (Adp)-Induced Platelet Aggregation With Rapid Onset And Offset Of Effects. In This Study,Synthesis Of Ticagrelor And Its Derivatives Has Been Accomplished In A Convergent Way. The Compound Design Was Based On Modifications Of Ticagrelor And Its Major Metabolite (33) In Order To Ameliorate Their Pharmacokinetic Properties And Dosing Profile. The Final Compounds (1A-G,35A-G) Were Evaluated For Their Inhibitory Effect On Adp-Induced Platelet Aggregation In Rats. The Assay Results Showed That Some Compounds (E. G.,1B,1D,33,35B,35F) Exhibited Comparable Potency With That Of Ticagrelor. (C) 2012 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2012.04.050

专利信息

专利号:US-9469614-B2
优先权日:2011-10-27
标 题:Synthesis of triazolopyrimidine compounds
发明人：ZUPANCIC BORUT; MARAS NENAD; STERK DAMJAN
权利人:LEK PHARMACEUTICALS
摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives.

专利号:EP-2607355-A1
优先权日:2011-12-23
标 题:Synthesis of triazolopyrimidine compounds
权利人:LEK PHARMACEUTICALS
摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor.

专利号:US-9278972-B2
优先权日:2011-12-23
标题 :Synthesis of triazolopyrimidine compounds
发明人：MARAS NENAD; GAZIC SMILOVIC IVANA; STERK DAMJAN
权利人:LEK PHARMACEUTICALS
摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor.

专利号:US-9221829-B2
优先权日:2011-09-14
标题:Synthesis of triazolopyrimidine compounds
发明人：MARAS NENED; ZUPANCIC BORUT
权利人:MARAS NENED; ZUPANCIC BORUT; LEK PHARMACEUTICALS
摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives, suitable for the preparation of Ticagrelor (TCG).

专利号:EP-2570405-A1
优先权日:2011-09-14
标题:Synthesis of Triazolopyrimidine Compounds
权利人:LEK PHARMACEUTICALS
摘要:The present invention relates to the filed of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives, suitable for the preparation of ticagrelor (TGC)

专利号:EP-2586773-A1
优先权日:2011-10-27
标题 :Synthesis of Triazolopyrimidine Compounds
权利人:LEK PHARMACEUTICALS
摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives.