📜Intepirdine中间体置于三氟乙酸体系中,用 二氯甲烷 作为反应溶剂,化学反应 2.0H,反应生成 3-苯磺酰基-8-(哌嗪-1-基)喹啉 参考文献:Syntheses,Radiolabelings,And In Vitro Evaluations Of Fluorinated Pet Radioligands Of 5-Ht6 Serotoninergic Receptors 标题:Syntheses,Radiolabelings,And In Vitro Evaluations Of Fluorinated Pet Radioligands Of 5-Ht6 Serotoninergic Receptors 摘要:The 5-Ht6 Receptors Are Potent Therapeutic Targets For Psychiatric And Neurological Diseases (Schizophrenia,Alzheimer'S Disease,Etc.). However,With Lack Of Specific Radiopharmaceuticals,Their Pharmacology Is Still Incomplete And Their Exploration Is Limited To Animal Models. In This Context,We Have Designed A Fluorinated Pet Radiotracer,[f-18]2Fnq1P,That Possesses A High Affinity And Selectivity For 5-Ht6. In Vitro Pet Autoradiographies In Rat Brain Sections With This Radiotracer Were In Accordance With The 5-Ht6 Distribution Pattern. DOI:10.1021/jm500372E
专利号:US-2008255359-A1 优先权日:2005-09-28 标题:Novel Chemical Process For the Synthesis of Quinoline Compounds 发明人:WADE CHARLES EDWARD 权利人:WADE CHARLES EDWARD 摘要:Disclosed is a novel, simplified and economic process for making 3-phenylsulphonyl quinolines with an amine group at position 8 of the quinoline ring system, including 3-phenylsulfonyl-8-piperazin-1-yl-quinoline in particular, in the absence of a palladium catalyst. Also disclosed is the crystallization of polymorphic forms of 3-phenylsulfonyl-8-piperazin-1-yl-quinoline.
专利号:EP-1928832-A1 优先权日:2005-09-28 标 题 :Novel chemical process for the synthesis of quinoline compounds
专利号:WO-2007039238-A1 优先权日:2005-09-28 标题 :Novel chemical process for the synthesis of quinoline compounds
专利号:US-9676772-B2 优先权日:2013-07-25 标题 :Pyrroloquinoline derivatives as 5-HT6 antagonists, preparation method and use thereof 发明人:ZAJDEL PAWEL; GRYCHOWSKA KATARZYNA; PAWLOWSKI MACIEJ; PARTYKA ANNA; WESOLOWSKA ANNA; BOJARSKI ANDRZEJ J; POPIK PIOTR; KOS TOMASZ; SATALA GRZEGORZ; LAMATY FREDERIC; COLACINO EVELINA; MARTINEZ JEAN; SUBRA GILLES; BANTREIL XAVIER 权利人:CENTRE NAT RECH SCIENT; UNIV MONTPELLIER; UNIV JAGIELLONSKI; INST FARMAKOLOGII POLSKIEJ AKADEMII NAUK; Uniwersyter Jagiellonski 摘要:This invention concerns pyrroloquinoline derivatives as antagonists of 5-HT6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in schizophrenia, anxiety, depression, maniac depression, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, panic attacks, attention deficit hyperactivity disorder, attention deficit disorder, Parkinson's disease, Huntington's disease, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, obesity and type-2 diabetes, functional bowel disorder, Irritable Bowel Syndrome. The compounds have the general formula (XIV), wherein the symbols have the meanings given in the description.
参考文献:10.1021/jm5003759 摘要:Krogsgaard-Larsen N, Jensen AA, Schrøder TJ, Christoffersen CT, Kehler J. Novel Aza-analogous Ergoline Derived Scaffolds as Potent Serotonin 5-HT6 and Dopamine D2 Receptor Ligands. J. Med. Chem. 2014 Jun 18;57(13):5823–8. doi: 10.1021/jm5003759. 参考文献:10.1007/s40120-018-0095-y 摘要:Andrews M, Tousi B, Sabbagh MN. 5HT6 Antagonists in the Treatment of Alzheimer’s Dementia: Current Progress. Neurology and Therapy. 2018 May 02;7(1):51–8. doi: 10.1007/s40120-018-0095-y.