3,4-二甲氧基苯甲醛肟置于sodium Tetrahydroborate,Amberlyst-15,Lithium Chloride体系中,化学反应 2.0H,以85%的收率获得产物3,4-二甲氧基苄胺 参考文献:Amberlyst-15(H+)-Nabh4-Licl: An Effective Reductor For Oximes And Hydrazones 标题:Amberlyst-15(H+)-Nabh4-Licl: An Effective Reductor For Oximes And Hydrazones 摘要:一种简单温和的过程在铬石15(H+)载体上使用氯化锂-氢化钠还原肟和肼,以高产率和纯度分别得到相应的胺和肼. DOI:10.1055/s-1999-2637
专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-2025049791-A1 优先权日:2023-08-03 标题:Synthesis of MEK7 Inhibitors and methods of Use Thereof 发明人:SCHEIDT KARL A; KIM DALTON ROBERT; ORR MEGHAN JO 权利人:UNIV NORTHWESTERN 摘要:Disclosed herein are 4-phenoxypyrimidine compounds and derivatives thereof for use as inhibitors of mitogen-activated protein kinase 7 (MEK7). The disclosed compounds and pharmaceutical compositions thereof may be used in methods for treating a disease or disorder associated with MEK7 activity, including cell proliferative diseases and disorders associated with MEK7 activity, such as cancer.
专利号:EP-3412666-A1 优先权日:2017-06-07 标 题:Process and intermediates for the preparation of bcl-2 inhibitors including venetoclax through reductive amination 发明人:GREGG BRIAN THOMAS; GEISS WILLIAM BERT; HERR ROBERT JASON 权利人:ALBANY MOLECULAR RES INC 摘要:The invention relates to a process for the preparation of compounds of formula (I), which are useful intermediates in the synthesis of Venetoclax and structurally related compounds, by reductive amination of a compound of formula (II).
专利号:US-9938282-B2 优先权日:2014-02-05 标 题:Expedient synthesis of sitagliptin 发明人:JANAGANI SATYANARAYANA; THADURI VENKATESHWAR KUMAR; VAMARAJU RAVISANKAR 权利人:STEREOKEM INC 摘要:Novel intermediates are disclosed as intermediates for preparation of a Sitagliptin. A novel synthetic method to prepare Sitagliptin using the said intermediates is also disclosed.
专利号:US-8017768-B1 优先权日:1990-09-01 标题:Catalitic synthesis of caged polynitramine compounds 发明人:NORRIS WILLIAM P; NIELSEN ARNOLD T 权利人:US NAVY 摘要:An improved method of preparing 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazaisowurtzitane (2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazatetracyclo[5.5.0.0 5,9 .0 3,11 ]dodecane) (HNIW) is disclosed. The compound is useful as a high energy, high density explosive or propellant oxidizer.
[参考文献]: J Ishida, Et Al. 3,4-Dimethoxybenzylamine As A Sensitive Pre-Column Fluorescence Derivatization Reagent For The Determination Of Serotonin In Human Platelet-Poor Plasma. J Chromatogr B Biomed Sci Appl. 1997 Apr 25;692(1):31-6. [参考文献]: J Ishida, Et Al. Spectrofluorimetric Determination Of 5-Hydroxyindoles With Benzylamine Or 3,4-Dimethoxybenzylamine As A Selective Fluorogenic Reagent. Analyst. 1991 Mar;116(3):301-4.
合成参考文献
摘要:Khartulyari, A.; Maier, M. E., Science of Synthesis Knowledge Updates, (2010) 3, 97. 摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 201. 摘要:Bagal, D. B.; Bhanage, B. M., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2018) 2, 383. 摘要:Bagal, D. B.; Bhanage, B. M., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2018) 2, 385. 摘要:Bagal, D. B.; Bhanage, B. M., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2018) 2, 387.