CAS: 220347-05-7; Ar-C 124910Xx

上下游产品

N-(((4S,5R)-2,2-dimethyl-5-vinyl-1 ,3-dioxolan-4-yl)methylene)-1-phenylmethanamine oxide trans-(1R,2R)-2-(3,4-difluorophenyl)cyclopropanecarboxylic acid (1R,2S)-2-(3,4-difluorophenyl)cyclopropanamine 4,6-dichloro-2-(propylsulfanyl)-5-pyrimidinamine(3aR,4S,6R,6aS)-6-(7-(((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-ol ticagrelor

1,2-二氟苯置于盐酸,Aluminum (III) Chloride,Sodium Hypochlorite,氯化亚砜,硼酸三甲酯,(S)-(+)-Alpha,Alpha-二苯基脯氨醇,Dimethyl Sulfide Borane,氨,水,N,N-二异丙基乙胺,Sodium Hydroxide,Sodium T-Butanolate体系中,用 四氢呋喃,甲醇,二氯甲烷,水,乙酸乙酯,甲苯 用作溶剂,化学反应 38.83H,反应生成去羟基乙氧基替格雷洛
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-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:US-2015005498-A1
优先权日:2011-09-14
标 题 :Synthesis of Triazolopyrimidine Compounds

专利号:WO-2013037942-A1
优先权日:2011-09-14
标题 :Synthesis of triazolopyrimidine compounds

专利号:EP-2755957-B1
优先权日:2011-09-14
标 题 :Synthesis of triazolopyrimidine compounds