📜吲哚-3-乙醛酰氯置于吡啶,Potassium Tert-Butylate体系中,用 四氢呋喃,甲醇,乙醚,二氯甲烷,水 用作溶剂,化学反应 21.5H,反应生成3-[1-[3-(二甲氨基)丙基]1H-吲哚-3-基]-4-(吲哚-3-基)1H-吡咯-2,5二酮 参考文献:A New,Efficient Method For The Synthesis Of Bisindolylmaleimides 标题:A New,Efficient Method For The Synthesis Of Bisindolylmaleimides 摘要: Doi:10.1021/jo980513C
专利号:US-5665877-A 优先权日:1993-12-07 标题:Synthesis of bisindolylmaleimides 发明人:FAUL MARGARET M; JIROUSEK MICHAEL R; WINNEROSKI II LEONARD L 权利人:LILLY CO ELI 摘要:The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.
专利号:US-5541347-A 优先权日:1993-12-07 标 题 :Synthesis of bisindolylmaleimides 发明人:FAUL MARGARET M; JIROUSEK MICHAEL R; WINNEROSKI II LEONARD L 权利人:LILLY CO ELI 摘要:The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.
专利号:US-7232842-B2 优先权日:2003-01-10 标题:Kinase inhibitors and associated pharmaceutical compositions and methods of use 发明人:WENDER PAUL A; SCANIO MARC J 权利人:UNIV LELAND STANFORD JUNIOR 摘要:The invention provides novel compounds useful as kinase inhibitors or as starting materials And/or intermediates in the synthesis of compounds useful as kinase inhibitors. The compounds have The general structure of formula (I) n nwherein A is a 3- to 8-membered ring, optionally substituted and/or heteroatom-containing, and R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X, Y, Z, p, and q are as defined herein. The compounds may also be in the form of a salt, ester, amide, or other analog. In preferred compounds, A is a 5- to 8-membered ring, R 1 is hydrogen, q is a bond, X is N, Y is Câ•?O, Z is N, R 2 contains a terminal amino moiety, p is 1, and R 3 and R 4 are linked to form a pyrrole ring fused to a second cyclic group. Pharmaceutical compositions and methods for using the compounds are also provided.
专利号:US-6133452-A 优先权日:1997-08-22 标题 :Synthesis of bisindolylmalimides 发明人:FAUL MARGARET MARY; WINNEROSKI JR LEONARD LARRY 权利人:LILLY CO ELI 摘要:The present invention provides for the reaction of optionally substituted indole-3-acetamides with optionally substituted methyl indole-3-glyoxyl reagent to prepare potent PKC inhibitors. The reaction is very efficient and robust macrocyclization methodology.
专利号:US-6229055-B1 优先权日:1996-04-12 标题 :Synthesis of fluorinated xanthene derivatives 发明人:KLAUBERT DIETER H; GEE KYLE R 权利人:MOLECULAR PROBES INC 摘要:Facile syntheses for fluorinated resorcinol and aminophenol derivatives are provided that yield isomer-free products in good yield. These novel methods use generally available precursors and standard laboratory reagents and equipment to reproducibly produce these synthetically useful reagents in relatively large quantities. The resulting fluorinated resorcinols and aniinophenols possess utility in the preparation of fluorinated fluorescein and rhodol dyes.
专利号:US-6037475-A 优先权日:1996-03-20 标题:Synthesis of indolymaleimides 发明人:FAUL MARGARET M; JIROUSEK MICHAEL R; MCDONALD III JOHN H; NEEL DAVID ANDREW 权利人:LILLY CO ELI 摘要:The present invention provides a method for synthesizing indolylmaleimides by reacting an activated maleimide preferably with an optionally substituted organometalic-3-indole in the presence of a transition metal catalyst.
1: Harmati G, Papp F, Szentandrássy N, Bárándi L, Ruzsnavszky F, Horváth B, Bányász T, Magyar J, Panyi G, Krasznai Z, Nánási PP. Effects of the PKC inhibitors chelerythrine and bisindolylmaleimide I (GF 109203X) on delayed rectifier K+ currents. Naunyn Schmiedebergs Arch Pharmacol. 2011 Feb;383(2):141-8. doi: 10.1007/s00210-010-0584-8. Epub 2010 Dec 1. 6: Grigorova-Borsos AM, Bakillah A, Urios P, Leblond V, Guillot R, Sternberg M. Production of type IV collagen and 72-kDa gelatinase by human endothelial cells cultured in high glucose. Effects of a protein kinase C inhibitor, GF 109203X. Biochem Cell Biol. 1996;74(5):659-67.
合成参考文献
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