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:US-7642369-B2 优先权日:2006-09-12 标 题 :Epoxyketone-based immunoproteasome inhibitors 发明人:KIM KYUNG BO; HO YIK KHUAN 权利人:UNIV KENTUCKY RES FOUND 摘要:An efficient new route for the preparation of dihydroeponemycin, an active eponemycin derivative, is provided, which includes the synthesis of the intermediate compound, a hydroxymethyl-substituted enone. In addition, a method is provided for synthesizing inhibitors, which includes PI′-modified analogues. These analogues selectively bind to a major immunoproteasome catalytic subunit LMP2 and inactivate its proteolytic activity in a method of treating diseases, including myeloma and other cancers, Huntington's disease and Alzheimer's disease.
专利号:US-4609643-A 优先权日:1980-08-06 标 题:Renin inhibitors, treatments and dipeptide synthesis 发明人:SZELKE MICHAEL; JONES DAVID M; HALLETT ALLAN 权利人:HAESSLE AB 摘要:Preparation of renin inhibitors based on the structure of natural renin substrate at residues 6 to 13 from the amino terminal thereof, the inhibitors being polypeptide analogues having in particular an isosteric non-peptide link corresponding to the 10, 11 peptide link of the substrate, and preparation of dipeptide analogues.
专利号:US-8129411-B2 优先权日:2005-12-30 标题:Organic compounds 发明人:EHARA TAKERU; GROSCHE PHILIPP; IRIE OSAMU; IWAKI YUKI; KANAZAWA TAKANORI; KAWAKAMI SHIMPEI; KONISHI KAZUHIDE; MOGI MUNETO; SUZUKI MASAKI; YOKOKAWA FUMIAKI 权利人:EHARA TAKERU; GROSCHE PHILIPP; IRIE OSAMU; IWAKI YUKI; KANAZAWA TAKANORI; KAWAKAMI SHIMPEI; KONISHI KAZUHIDE; MOGI MUNETO; SUZUKI MASAKI; YOKOKAWA FUMIAKI; NOVARTIS AG 摘要:The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. n The compounds have the formula I′ n nwherein R1, R2, T, R3 and R4 are as defined in the specification.
参考标题:Hydrodehalogenation Of Alkyl Iodides With Base-Mediated Hydrogenation And Catalytic Transfer Hydrogenation: Application To The Asymmetric Synthesis Of N-Protected α-Methylamines 作者:Pijus K. Mandal,J. Sanderson Birtwistle,John S. Mcmurray |发布日期:2014.9.5 摘要:We Report A Very Mild Synthesis Of N-Protected α-Methylamines From The Corresponding Amino Acids. Carboxyl Groups Of Amino Acids Are Reduced To Iodomethyl Groups Via Hydroxymethyl Intermediates. Reductive Deiodination To Methyl Groups Is Achieved By Hydrogenation Or Catalytic Transfer Hydrogenation Under Alkaline Conditions. Basic Hydrodehalogenation Is Selective For The Iodomethyl Group Over Hydrogenolysis-Labile
合成参考文献
参考文献:10.1055/s-0039-1691500 摘要:Deng J, Long X, Ding Y, Wu H. Total Synthesis of Asperchalasine A. Synlett. 2019 Dec 13;31(04):301–8. doi: 10.1055/s-0039-1691500. 参考文献:10.1055/s-0037-1611235 摘要:Synthesis of (–)-Asperchalasine A. Synfacts. 2018 Oct 18;14(11):1111. doi: 10.1055/s-0037-1611235.