专利号:US-6271379-B1 优先权日:2000-03-08 标题:Intermediates useful for the synthesis of huperzine A 发明人:TUECKMANTEL WERNER; KOZIKOWSKI ALAN P 权利人:UNIV GEORGETOWN 摘要:Intermediates useful for the synthesis of huperzine A represented by the structures below, n and methods for their synthesis, wherein: n R 1 is lower alkyl, benzyl, or substituted benzyl; n X is a suitable leaving group; n Y is an electron withdrawing group that can subsequently be converted into an amino group; n one broken line is present as a carbon—carbon bond and the other broken line is absent, where the broken line forms an unconjugated carbon—carbon double bond, which double bond may be endocyclic whereby n is 3 or the double bond may be exocyclic whereby n is 2.
专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:EP-0747486-B1 优先权日:1995-06-07 标题:Microbiological method for the synthesis of heteroaromatic caboxylic acids using microorganisms of the genus Alcaligenes
专利号:WO-0166524-A2 优先权日:2000-03-08 标题:Intermediates useful for the synthesis of huperzine a
专利号:EP-0747486-A1 优先权日:1995-06-07 标 题:Microbiological method for the synthesis of heteroaromatic caboxylic acids using microorganisms of the genus Alcaligenes
[参考文献]: Jennifer A Jacobsen, Et Al. Identifying Chelators For Metalloprotein Inhibitors Using A Fragment-Based Approach. J Med Chem. 2011 Jan 27;54(2):591-602.
合成参考文献
摘要:Jiao, N.; Li, Z., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 705. 参考文献:10.1107/s1600536810030916 摘要:Hemamalini M, Fun HK. 2-Amino-5-bromo-pyridinium 6-oxo-1,6-dihydro-pyridine-2-carboxyl-ate monohydrate. Acta Crystallogr Sect E Struct Rep Online. 2010 Aug 11;66(Pt 9):o2246–7. 参考文献:10.1107/s1600536810032307 摘要:Hemamalini M, Fun HK. 2-Amino-5-chloro-pyridinium 6-oxo-1,6-dihydro-pyridine-2-carboxyl-ate 0.85-hydrate. Acta Crystallogr Sect E Struct Rep Online. 2010 Aug 18;66(Pt 9):o2338.