3,3-Ethylenedioxy-5α-Hydroxy-17α-Acetoxy-11β-4-(N,,N-Dimethylaminophenyl)-19-Norpregna-9-En-20-One置于水,碘,溶剂黄146,1,2-二溴乙烷体系中,用 四氢呋喃 用作溶剂,化学反应 2.5H,以82%的收率获得醋酸乌利司他 参考文献: Method For Preparing 17 Alpha-Acetoxy-11Beta-(4-N,N-Dimethylaminophenyl)-19-Norpregna-4,9-Diene-3,20-Dione,Intermediates Thereof,And Methods For The Preparation Of Such Intermediates[fr] Procede De Preparation De 17 Dollar G(A)-Acetoxy-11 Dollar G(B)-(4-N,N-Dimethylaminophenyl)-19-Norpregna-4,9-Diene-3,20-Dione,D'Intermediaires De Ceux-Ci Et Procedes De Preparation Desdits Intermediaires 标题: Method For Preparing 17 Alpha-Acetoxy-11Beta-(4-N,N-Dimethylaminophenyl)-19-Norpregna-4,9-Diene-3,20-Dione,Intermediates Thereof,And Methods For The Preparation Of Such Intermediates[fr] Procede De Preparation De 17 Dollar G(A)-Acetoxy-11 Dollar G(B)-(4-N,N-Dimethylaminophenyl)-19-Norpregna-4,9-Diene-3,20-Dione,D'Intermediaires De Ceux-Ci Et Procedes De Preparation Desdits Intermediaires
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-11993606-B2 优先权日:2015-10-16 标题:Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof 发明人:MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; PANGAN AILEEN L; SONG IN-HO; KLÜNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S 权利人:ABBVIE INC 摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).
专利号:US-11976077-B2 优先权日:2015-10-16 标 题 :Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms therof 发明人:PANGAN AILEEN L; TEIXEIRA HENRIQUE D; MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; KLÜNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S 权利人:ABBVIE INC 摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and atopic dermatitis), kits, methods of synthesis, and products-by-process.
专利号:US-11512092-B2 优先权日:2015-10-16 标题 :Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof 发明人:ALLIAN AYMAN; JAYANTH JAYANTHY; MOHAMED MOHAMED-ESLAM F; MULHERN MATHEW; NORDSTROM FREDRIK LARS; OTHMAN AHMED A; ROZEMA MICHAEL J; BHAGAVATULA LAKSHMI; MARROUM PATRICK J; MAYER PETER T; SHEIKH AHMAD Y; BORCHARDT THOMAS B; KLÜNDER BEN 权利人:ABBVIE INC 摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).
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
1: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Ulipristal. 2022 Jul 18. 11(4):198-202. doi: 10.4103/gmit.gmit_95_21. 3: Glasier AF, Cameron ST, Fine PM, Logan SJ, Casale W, Van Horn J, Sogor L, Blithe DL, Scherrer B, Mathe H, Jaspart A, Ulmann A, Gainer E. Ulipristal acetate versus levonorgestrel for emergency contraception: a randomised non- inferiority trial and meta-analysis. Lancet. 2010 Feb 13;375(9714):555-62. doi: 10.1016/S0140-6736(10)60101-8. Epub 2010 Jan 29. Erratum in: Lancet. 2014 Oct 25;384(9953):1504. 12(10):e0186158. doi: 10.1371/journal.pone.0186158. 5: Vitale SG, Ferrero S, Caruso S, Barra F, Marín-Buck A, Vilos GA, Vitagliano A, Török P, Ciebiera M, Cianci A. Ulipristal Acetate Before Hysteroscopic Myomectomy: A Systematic Review. Obstet Gynecol Surv. 2020 Feb;75(2):127-135. doi: 10.1097/OGX.0000000000000764. 2019 Feb 12. 77(15):1665-1675. doi: 10.1007/s40265-017-0812-3. 39(6):230-231. doi: 10.18773/austprescr.2016.091. Epub 2016 Dec 5.
合成参考文献
摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198