11β-(4-N,N-Dimetnylaminophenyl)-17α-Ethynyl-17β-Hydroxy-Estra-4,9-Diene-3-One置于溶剂黄146,三乙胺体系中,用 甲醇,二氯甲烷,水 用作溶剂,化学反应 7.5H,反应生成醋酸乌利司他中间体 参考文献: Novel Process And Intermediate For Preparation Of Ulipristal[fr] Nouveau Procédé Et Nouvel Intermédiaire Pour Préparation D'Ulipristal 标题: Novel Process And Intermediate For Preparation Of Ulipristal[fr] Nouveau Procédé Et Nouvel Intermédiaire Pour Préparation D'Ulipristal 摘要:本发明涉及一种用于制备尤利普利斯塔尔(i)的新型工艺,该工艺包括将17-α-乙炔基-17-β-羟基-11-β-(4-N,N-二甲胺基苯基)-9-诺孕烯-4,9-二烯-3-酮(III)与苯基亚砜氯化物(iva)或对硝基苯基亚砜氯化物(ivb)在有机碱和溶剂存在下反应,分别得到亚砜氧化物(va)或(vb).亚砜氧化物(va)或(vb)与醇性溶剂中的碱金属烷氧化物反应,随后经过水酸处理.本发明还涉及新型中间体11-β-(4-N,N-二甲基氨基苯基)-21(对硝基苯基亚砜基)-19-诺孕烯-4(5),9(10),17(20) 20-四烯-3-酮(vb).
专利号:US-8110691-B2 优先权日:2006-06-14 标题 :Industrial process for the synthesis of 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione and new intermediates of the process 发明人:DANCSI LAJOSNE; VISKY GYOERGY; TUBA ZOLTAN; CSOERGEI JANOS; MOLNAR CSABA; MAGYARI ENDRENE 权利人:DANCSI LAJOSNE; VISKY GYOERGY; TUBA ZOLTAN; CSOERGEI JANOS; MOLNAR CSABA; MAGYARI ENDRENE; RICHTER GEDEON NYRT 摘要:A new industrial process for the synthesis of solvate-free 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB-2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII) and (VIII) used as intermediates in the process.
专利号:US-9676814-B2 优先权日:2013-10-01 标题:Industrial process for the synthesis of ulipristal acetate and its 4′-acetyl analogue 发明人:Mahó Sándor; SÃ?NTA CSABA; Csörgei János; Horváth János; ARANYI ANTAL; BÉNI ZOLTÃ?N 权利人:RICHTER GEDEON NYRT 摘要:The present invention relates to a new process for the synthesis of compounds of formula (I) (wherein the meaning of R is dimethylamino or acetyl group) using the compound of formula (II) (wherein the meaning of R is dimethylamino or 2-methyl-1,3-dioxolan-2-yl group) as starting material, as well as to the intermediate of the process.
专利号:US-2009187032-A1 优先权日:2006-06-14 标 题 :INDUSTRIAL PROCESS FOR THE SYNTHESIS OF 17alpha-ACETOXY-11beta-[4-(N,N-DIMETHYL-AMINO)-PHENYL]-19-NORPREGNA-4,9-DIENE-3,20-DIONE AND NEW INTERMEDIATES OF THE PROCESS
专利号:EP-3052513-B1 优先权日:2013-10-01 标 题:Industrial process for the synthesis of ulipristal acetate and its 4'-acetyl analogue
专利号:EP-2027140-B1 优先权日:2006-06-14 标题:Industrial process for the synthesis of 17 alpha -acetoxy-11 beta -[4-(n,n-dimethyl-amino)- phenyl]-19-norpregna-4,9-diene-3,20-dione and new intermediates of the process
专利号:EP-3052513-A1 优先权日:2013-10-01 标题 :Industrial process for the synthesis of ulipristal acetate and its 4'-acetyl analogue
1: Haeger KO, Lamme J, Cleland K. State of emergency contraception in the U.S., 2018. Contracept Reprod Med. 2018 Sep 5;3:20. doi: 10.1186/s40834-018-0067-8. eCollection 2018. Review. 2: Donnez J. Liver injury and ulipristal acetate: an overstated tragedy? Fertil Steril. 2018 Sep;110(4):593-595. doi: 10.1016/j.fertnstert.2018.06.044. e2. doi: 10.1016/j.jogc.2018.05.020. Review. doi: 10.1097/MD.0000000000011532. 7: Gan N, Sun Q, Zhang M, Tang P, Zhao L, Xie T, Zhang Y, Li H. Insights into the interaction of ulipristal acetate and human serum albumin using multi-spectroscopic methods, molecular docking, and dynamic simulation. J Biomol Struct Dyn. 2018 Jul
合成参考文献
参考文献:10.1016/s0140-6736(10)60146-8 摘要:Benagiano G, von Hertzen H. Towards more effective emergency contraception Lancet. 2010 Feb 13;375(9714):527–8. doi: 10.1016/s0140-6736(10)60146-8.