顺丁烯二酸 在 甲烷体系中,用 乙醇作为反应溶剂,反应 2.75H,获得 Asenapine Maleate 参考文献:Intermediate Compounds For The Preparation Of Trans-5-Chloro-2-Methyl-2,3,3A,12B-Tetrahydro-1H-Dibenz[2,3:6,7]Oxepino[4,5-C]Pyrrole 标题:Intermediate Compounds For The Preparation Of Trans-5-Chloro-2-Methyl-2,3,3A,12B-Tetrahydro-1H-Dibenz[2,3:6,7]Oxepino[4,5-C]Pyrrole
专利号:US-2013274466-A1 优先权日:2010-09-27 标 题:Process for the preparation of tetracyclic derivatives and intermediate products used in the process 发明人:GORIN BORIS; DIXON CRAIG EDWARD; QU YANG 权利人:GORIN BORIS; DIXON CRAIG EDWARD; QU YANG; ALPHORA RES INC 摘要:A process for preparation of a compound of formula I or a pharmaceutically acceptable salt thereof, is disclosed. The process involves subjecting a compound of formula II to Ullmann-type conditions to effect an intra-molecular ring closure reaction to form the compound of formula I. The different substituents are as described in the specification. Further, the process can provide an alternate route for the synthesis of asenapine from starting materials that can be readily available.
专利号:US-9751877-B2 优先权日:2012-09-21 标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders 发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-9505771-B2 优先权日:2011-05-18 标 题 :Stable micronised monoclin form of asenapine maleate and its synthesis 发明人:BERTRAN AGUSTI; TERRADAS JOSEP 权利人:BERTRAN AGUSTI; TERRADAS JOSEP; LABORATORIES LESVI S L 摘要:A stable micronized monoclinic form of asenapine maleate is described, which comprises 5% by weight or less of orthorhombic form or any other crystalline form of asenapine maleate, wherein the asenapine maleate has a particle size distribution characterized by a d90 equal to or below 40 μm. Processes for preparing the stable micronized monoclinic form of asenapine maleate are also described. Formula (I).
专利号:RU-2397164-C2 优先权日:2005-04-07 标题:INTERMEDIATE COMPOUNDS FOR SYNTHESIS OF TRANS-5-CHLORO-2-METHYL-2,3,3a,12b-TETRAHYDRO-1H-DIBENZ[2,3:6,7]-OXEPINO[4,5-c]PYRROLE
专利号:WO-2012172449-A1 优先权日:2011-06-13 标题:Lactams as beta secretase inhibitors 发明人:BRODNEY MICHAEL AARON 权利人:PFIZER; BRODNEY MICHAEL AARON 摘要:Compound and pharmaceutically acceptable salts of the compound are disclosed, wherein the compound has the structure (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. The compound of formula I is useful as beta secretase inhibitor for use in the treatment of Alzheimer's and other neurodegenerative and/or neurological disorders.
专利号:US-2016229847-A1 优先权日:2013-10-04 标 题:Novel bicyclic pyridinones as gamma-secretase modulators 发明人:PETTERSSON MARTIN YOUNGJIN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; JOHNSON DOUGLAS SCOTT; KAUFFMAN GREGORY WAYNE; O'DONNELL CHRISTOPHER WILLIAM; PATEL NANDINI CHATURBHAI; STEPAN ANTONIA FRIEDERIKE; STIFF CORY MICHAEL; SUBRAMANYAM CHAKRAPANI; TRAN TUAN PHONG; VERHOEST PATRICK ROBERT 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula II as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
1: Wulff S, Nielsen J, Pedersen N, Nielsen MØ. Asenapine-induced severe dystonia in a patient with schizophrenia: medication error due to sound-alike drug. BMJ Case Rep. 2025 Jun 24;18(6):e264354. doi: 10.1136/bcr-2024-264354. 2: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Asenapine. 2025 Mar 15. 182:117756. doi: 10.1016/j.biopha.2024.117756. Epub 2024 Dec 17. 14(1):28225. doi: 10.1038/s41598-024-79372-5.
合成参考文献
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