专利号:US-9783549-B2 优先权日:2013-11-04 标题:Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin B 发明人:FANG FRANCIS G; KIM DAE-SHIK; CHOI HYEONG-WOOK; CHASE CHARLES E; LEE JAEMOON 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
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-8309599-B2 优先权日:2006-09-08 标题 :Synthesis of FR901464 and analogs with antitumor activity 发明人:KOIDE KAZUNORI; ALBERT BRIAN J; SIVARAMAKRISHNAN ANANTHAPADMANABHAN 权利人:KOIDE KAZUNORI; ALBERT BRIAN J; SIVARAMAKRISHNAN ANANTHAPADMANABHAN; UNIV PITTSBURGH 摘要:The present invention provides novel analogs of FR901464, as well as an improved methodology for preparing FR901464 and its analogs. These compounds display an anti-cancer activity and are candidates for therapies against a number of disease states associated with dysfunctional RNA splicing.
专利号:US-9006472-B2 优先权日:2011-11-17 标 题 :Methods for the synthesis of 13C labeled plasmalogen 发明人:KHAN M AMIN; WOOD PAUL L; GOODENOWE DAYAN 权利人:PHENOMENOME DISCOVERIES INC 摘要:A method for preparing 13 C labeled plasmalogens as represented by Formula B: n n n n n n n n n n The method involves producing a 13 C labeled cyclic plasmalogen precursor of Formula A: n nand conversion of the precursor to a plasmalogen of Formula B.
专利号:US-9012704-B2 优先权日:2011-11-17 标题 :Methods for the synthesis of 13C labeled iodotridecane and use as a reference standard 发明人:KHAN M AMIN; WOOD PAUL L; GOODENOWE DAYAN 权利人:PHENOMENOME DISCOVERIES INC 摘要:A method for preparing 13 C labeled iodotridecane represented by Formula A: n nThe method comprises the conversion of 13 C labeled propargyl alcohol to 13 C labeled iodotridecane via alkylation of propargyl alcohol with iododecane.
专利号:US-5446062-A 优先权日:1993-11-12 标 题:((4-alkoxypyran-4-yl) substituted) ether, arylalkyl-, arylalkenyl-, and arylalkynyl)urea inhibitors of 5-lipoxygenase 发明人:DELLARIA JOSEPH F; BASHA ANWER; BLACK LAWRENCE A; CHERNESKY LINDA J; LEE WENDY 权利人:ABBOTT LAB 摘要:Compounds of the structure where W is selected from where Q is oxygen or sulfur, R6 and R7 are hydrogen or alkyl, or R6 and R7, together with the nitrogen atoms to which they are attached, define a radical of formula Z is -CH2-, oxygen, sulfur, or -NR9, L1 and L2 are selected from a valence bond, alkylene, propenylene, and propynylene; R1 and R2 are independently selected from alkyl, alkoxy, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl; Y is selected from oxygen, >NR10, and L3 is selected from alkylene of one to three carbon atoms, propenylene, propynylene, and R3, R4, and R5 are hydrogen or alkyl of one to four carbon atoms inhibit the synthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
参考标题:Novel And Efficient Synthesis Of Iminocoumarins Via Copper-Catalyzed Multicomponent Reaction 作者:Sun-Liang Cui,Xu-Feng Lin,Yan-Guang Wang |发布日期:2006.9.1 摘要:A Variety Of Substituted Iminocoumarins Are Prepared In Good To Excellent Yields Via A Copper-Catalyzed Multicomponenet Reaction Of Sulfonyl Azides, Terminal Alkynes, And Salicylaldehydes Or O-Hydroxylacetophenones. The Method Is General, Mild, Versatile, And Efficient. A Plausible Mechanism For The Domino Process Is Proposed.
合成参考文献
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