合成目标产物 Rivaroxaban 主要起始原料 5-Chlorothiophene-2-Carbonyl Chloride And 3-Morpholinone, 4-[4-[(5S)-5-(Aminomethyl)-2-Oxo-3-Oxazolidinyl]Phenyl]-, Methanesulfonate (1:1)
898543-06-1 + 24065-33-6 + 593-51-1 = 366789-02-8 + 97799-98-9 反应条件:1.1 Reagents: 1,1′-Carbonyldiimidazole Solvents: Dimethylformamide; 30 Min,25 °C1.2 4 H,34 °C 标题:Method For Producing An Intermediate Of Rivaroxaban 参考文献:Japan]
446292-08-6 = 366789-02-8 + 97799-98-9 反应条件:1.1 Solvents: Acetonitrile,Water; Rt -> 40 °C; 2 H,40 °C; 40 °C -> 33 °C1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 5.7,33 °C2.1 Reagents: 1,1′-Carbonyldiimidazole Solvents: Dimethylformamide; 30 Min,25 °C2.2 4 H,34 °C 标题:Method For Producing An Intermediate Of Rivaroxaban 参考文献:Japan
5-Chloro-N-[(5S)-2-Oxo-3-[4-(3-Oxo-4-Morpholinyl)Phenyl]-1,3-Oxazolin-5-Yl]Methyl-N'-Benzyl-2-Thiophene Carboxamide 以54.3的收率获得产物利伐沙班 参考文献: Processes For The Preparation Of 5-Chloro-N-({(5S)-2-Oxo-3-[4-(3-Oxo-4-Morpholinyl)Phenyl]-1,3-Oxazolidin-5-Yl}Methyl)-2-Thiophene-Carboxamide And Intermediates Thereof[fr] Procédés De Préparation De 5-Chloro-N-({(5S)-2-Oxo-3-[4-(3-Oxo-4-Morpholinyl)Phényl]-1,3-Oxazolidin-5-Yl Méthyl)-2-Thiophène-Carboxamide Et De Ses Intermédiaires 标题: Processes For The Preparation Of 5-Chloro-N-({(5S)-2-Oxo-3-[4-(3-Oxo-4-Morpholinyl)Phenyl]-1,3-Oxazolidin-5-Yl}Methyl)-2-Thiophene-Carboxamide And Intermediates Thereof[fr] Procédés De Préparation De 5-Chloro-N-({(5S)-2-Oxo-3-[4-(3-Oxo-4-Morpholinyl)Phényl]-1,3-Oxazolidin-5-Yl Méthyl)-2-Thiophène-Carboxamide Et De Ses Intermédiaires 摘要:本发明涉及制备噁唑烷酮衍生物的过程.更具体地,本发明提供了制备5-氯-N-({(5S)-2-氧代-3-[4-(3-氧代-4-吗啡基)苯基]-1,3-噁唑烷-5-基甲基}-2-噻吩羧酰胺及其中间体的过程.其中l是离去基,如卤素原子(f,Cl,Br,I)或-Oso2R,其中r = C'-4烷基直链或支链,取代或未取代芳基,取代或未取代芳基烷基;使用适当的试剂反应,以提供式(II)的化合物.反应步骤通过将式(iv)的化合物与胺源反应来完成,胺源可以溶解在水或醇等溶剂中,例如氢氧化铵.
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:US-9233989-B2 优先权日:2011-10-11 标题:Sila analogs of oxazolidinone derivatives and synthesis thereof 发明人:REDDY DUMBALA SRINIVASA; BALAMKUNDU SEETHARAM SINGH; RAMESH REMYA 权利人:COUNCIL SCIENT IND RES 摘要:The invention discloses silaanalogs of oxazolidinone compounds, to pharmaceutical compositions and to the synthesis of the oxazolidinone derivatives of formula I. The invention further relates to methods of treating a subject suffering with gram positive pathogens including those resistant to methicillin and vancomycin using the compound(s) or modulation of coagulation properties of blood-clotting cascade or compositions of the oxazolidinone derivatives of the invention.
专利号:US-11891384-B2 优先权日:2017-01-04 标题:Process for the preparation of Rivaroxaban involving novel intermediate 发明人:SATHE DHANANJAY G; DAS ARIJIT; Raikar Sanjay; SURVE YASHWANT S; PANDIT BHUSHAN S 权利人:UNICHEM LAB LTD 摘要:The present invention relates to the novel key intermediate, 4-{4-[(SS)-(Aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]-phenyl}-morpholin-3-one perchlorate, m the synthesis of rivaroxaban. The invention further relates to the crystalline form of novel intermediate, the process to prepare the novel intermediate and method of preparing rivaroxaban using this novel intermediate. The invention provides an improved and efficient process for preparation of Rivaroxaban.
专利号:US-2024368164-A1 优先权日:2021-04-28 标 题 :Purine nucleosides, their intermediates, and methods of preparation thereof 发明人:RAVI RAMA SURESH; JACOBSON KENNETH A; POE RUSSELL BIRCH 权利人:ASTROCYLE PHARMACEUTICALS INC; US HEALTH 摘要:The present invention provides purine nucleoside analog compounds and methods of use thereof for treatment of certain injuries, disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries. The present invention further provides methods of synthesizing such compounds, and intermediates useful in the synthesis of such compounds.
专利号:WO-2013046211-A1 优先权日:2011-09-27 标 题 :Processes for the preparation of 5-chloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl) phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide and intermediates thereof 发明人:MOHAN RAO DODDA; KRISHNA REDDY PINGILI; VENKAT REDDY BUTHUKURI 权利人:SYMED LABS LTD; MOHAN RAO DODDA; KRISHNA REDDY PINGILI; VENKAT REDDY BUTHUKURI 摘要:TThe present invention provides processes for the preparation of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide (I) and intermediates thereof. Also provides novel intermediates and their use in the synthesis of oxazolidine derivatives.
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.
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合成参考文献
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