专利号:US-7652137-B2 优先权日:2003-03-06 标 题:Synthesis of 5 substituted 7-azaindoles and 7-azaindolines 发明人:GRACZYK PIOTR PAWEL; KHAN AFZAL; BHATIA GURPREET SINGH 权利人:EISAI R&D MAN CO LTD 摘要:The present invention provides a novel substituted azaindoline intermediate of formula (I) and a method for its synthesis. The novel substitued azaindoline intermediate (I) is provided for use in the manufacture of 5-substituted 7-azaindolines and 5-substituted 7-azaindoles.
专利号:US-9790207-B2 优先权日:2015-09-04 标题 :Pan-genomic inhibitors of NS5A protein encoded by HCV, pharmaceutical compositions, intermediates for inhibitor synthesis, and their synthesis and application methods 发明人:IVACHTCHENKO ALEXANDRE VASILIEVICH; MITKIN OLEG DMITRIEVICH 权利人:IVACHTCHENKO ALEXANDRE VASILIEVICH; IVASHCHENKO ANDREY ALEXANDROVICH; SAVCHUK NIKOLAY FILIPPOVICH; ALLA CHEM LLC 摘要:Compound represented by formula 1: n nor a pharmaceutically acceptable salt, a hydrate, a crystalline form, or a stereoisomer thereof, wherein:n nR1 is hydrogen, tert-butoxycarbonyl,n n nwhere R11 is an optionally substituted C 1 -C 6 alkyl, an optionally substituted C 3 -C 6 cycloalkyl, or an optionally substituted C 1 -C 6 alkyloxy, and arrows (â†?) indicate the position of substituents attachment;n nR2 is hydrogen, halogen, or C 1 -C 4 alkyl;n nR3 is an optionally substituted aryl, an optionally substituted aryloxy, an optionally substituted arylsulfanyl, an optionally substituted arylamino, or an optionally substituted nitrogen hetaryl;n n n n n n n n n n n n n where R41 is an optionally substituted C 1 -C 6 alkyl, an optionally substituted C 3 -C 6 cycloalkyl, or an optionally substituted C 1 -C 6 alkyloxy; X is buta-1,3-diynylene or 1,4-phenylene; arrows (â†?) indicate the position of substituents attacment.
专利号:US-8404670-B2 优先权日:2009-02-11 标题:Histamine H3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SPEAR KERRY L 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SPEAR KERRY L; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
专利号:CN-101234996-B 优先权日:2008-02-29 标题:A kind of green synthesis method of ketazine
专利号:CN-109422662-B 优先权日:2017-08-25 标题:Synthesis method of N-phenyl acetamide compound
专利号:CN-111039796-A 优先权日:2019-12-12 标 题 :Novel synthesis method of 4' -chloro-2-aminobiphenyl
[参考文献]: G Shtacher, Et Al. Synthesis Of Chelating Compounds To Be Used As Potential Bone Seekers. J Med Chem. 1966 Mar;9(2):197-203.
合成参考文献
摘要:Griesbeck, A. G.; Soldevilla, A., Science of Synthesis, (2008) 43, 349. 摘要:Ulrich, H., Science of Synthesis Knowledge Updates, (2010) 1, 401. 摘要:Sanford, M. S.; Cook, A., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 199. 摘要:Ros, A.; Fernández, R.; Lassaletta, J. M., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 431.