5-溴-2-氟苯甲醛置于1,8-二氮杂双环[5.4.0]十一碳-7-烯,三乙胺,Potassium Hydroxide体系中,用 乙醇,N,N-二甲基乙酰胺,水,二甲基亚砜 作为反应溶剂,化学反应 7.0H,反应生成 5-溴苯并[b]噻吩 参考文献:Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines And Tetraoxanes Potential Two-Stage Antimalarials 标题:Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines And Tetraoxanes Potential Two-Stage Antimalarials 摘要:The Syntheses And Antiplasmodial Activities Of Various Substituted Aminoquinolines Coupled To An Adamantane Carrier Are Described. The Compounds Exhibited Pronounced In Vitro And In Vivo Activity Against Plasmodium Berghei In The Thompson Test. Tethering A Fluorine Atom To The Aminoquinoline C(3) Position Afforded Fluoroaminoquinolines That Act As Intrahepatocytic Parasite Inhibitors,With Compound 25 Having An Ic50 = 0.31 Mu M And Reducing The Liver Load In Mice By Up To 92% At 80 Mg/kg Dose. Screening Our Peroxides As Inhibitors Of Liver Stage Infection Revealed That The Tetraoxane Pharmacophore Itself Is Also An Excellent Liver Stage P. Berghei Inhibitor (78: Ic50 = 0.33 Mu M). Up To 91% Reduction Of The Parasite Liver Load In Mice Was Achieved At 100 Mg/kg. Examination Of Tetraoxane 78 Against The Transgenic 3D7 Strain Expressing Luciferase Under A Gametocyte-Specific Promoter Revealed Its Activity Against Stage Iv-V Plasmodium Falciparum Gametocytes (Ic50 = 1.16 +/-0.37 Mu M). To The Best Of Our Knowledge,Compounds 25 And 78 Are The First Examples Of Either An 4-Aminoquinoline Or A Tetraoxane Liver Stage Inhibitors. DOI:10.1021/acs.Jmedchem.5B01374
专利信息
专利号:CN-108373416-B 优先权日:2018-04-28 标 题 :A kind of method of photo/nickel synergistic catalysis synthesis of diarylamine
专利号:US-9351954-B2 优先权日:2009-12-04 标 题:Multicyclic compounds and methods of use thereof 发明人:SHAO LIMING; CAMPBELL JOHN EMMERSON; HEWITT MICHAEL CHARLES; CAMPBELL UNA; HANANIA TALEEN G 权利人:SUNOVION PHARMACEUTICALS INC; PGI DRUG DISCOVERY LLC 摘要:Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. For example, disclosed herein are compounds having formula (IIa) shown below, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein the variables are defined herein. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
专利号:CN-117466744-A 优先权日:2023-11-02 标 题:A method for photochemical iron-catalyzed synthesis of aromatic amine compounds
专利号:US-2007275968-A1 优先权日:2004-09-07 标 题 :Substituted Biphenyl Derivative 发明人:KURATA HITOSHI; NISHIMATA TOYOKI; WATANABE YUKIKO; EBISAWA MASAYUKI; FUJIMOTO TEPPEI; KOBAYASHI HIDEKI 权利人:KURATA HITOSHI; NISHIMATA TOYOKI; WATANABE YUKIKO; EBISAWA MASAYUKI; FUJIMOTO TEPPEI; KOBAYASHI HIDEKI 摘要:The present invention relates to a biaryl derivative or a pharmacologically acceptable salt thereof having an excellent collagen-synthesis inhibition activity. A biaryl derivative having a structure represented by the following General Formula (I) or a pharmacologically acceptable salt thereof: n nwherein n R 1 represents a C 6 -C 10 aryl group which is substituted with one to three group(s) each independently selected from the group consisting of a group defined by formula R-L-, a di-(C 1 -C 6 alkyl)amino group, a di-(C 1 -C 6 alkyl)aminosulfonyl group, a hydroxyaminocarbonyl group, and a halogen atom, and so on; R represents a C 1 -C 6 alkyl group, and so on; L represents a sulfonyl group, an aminosulfonyl group, or a sulfonylamino group, and so on; R 2 represents a hydrogen atom, and so on; A represents a group defined by formula (II), (III), or (IV); R 3 represents a C 1 -C 6 alkyl group, and so on; and R 4 represents a C 1 -C 6 alkyl group, and so on.
专利号:US-9695191-B2 优先权日:2009-08-05 标题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN 权利人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN; POLYPHOR AG 摘要:Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT 2B (5-HT 2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.
专利号:US-2010117066-A1 优先权日:2007-04-28 标题:Organic Semiconductors 发明人:HEENEY MARTIN; ZHANG WEINMIN; MCCULLOOCH IAIN 权利人:MERCK PATENT GMBH 摘要:The invention relates to novel substituted dibenzo[d,d′]benzo[1,2-b;4,5-b′]dithiophenes (DBBDT), to methods of their synthesis, to organic semiconducting materials, formulations and layers comprising them, and to electronic devices, like organic field effect transistors (OFETs), comprising them.
摘要:Davies, G. H. M.; Wisniewski, S. R., Science of Synthesis Knowledge Updates, (2021) 2, 194. 摘要:Yoshikai, N.; Rayner, C. M.; Graham, M. A., Science of Synthesis Knowledge Updates, (2020) 2, 94. 摘要:Yoshikai, N.; Rayner, C. M.; Graham, M. A., Science of Synthesis Knowledge Updates, (2020) 2, 121. 摘要:Sawamura, M.; Shimizu, Y., Science of Synthesis: Knowledge Updates, (2024) 2, 212.