专利号:US-6358928-B1 优先权日:1999-11-22 标 题 :Peptidyl sulfonyl imidazolides as selective inhibitors of serine proteases 发明人:RASNICK DAVID W 权利人:ENZYME SYSTEMS PRODUCTS 摘要:Novel alpha-amino and peptidyl sulfonyl imidazolides, a method for their synthesis, and a method for inhibiting serine proteases therewith are disclosed. Pharmaceutical compositions containing alpha-amino and peptidyl sulfonyl imidazolides and their use in the treatment of disease states characterized by an over-activity of serine proteases are also disclosed. Novel synthetic methods for the synthesis of sulfonyl derivatives, particularly alpha-amino and peptidyl sulfonyl derivatives, from thioic acid S-esters are also disclosed.
专利号:US-4978744-A 优先权日:1989-01-27 标题:Synthesis of dolastatin 10 发明人:PETTIT GEORGE R; SINGH SHEO B 权利人:UNIV ARIZONA 摘要:A complicated but extremely important scheme of synthesis has been developed for synthesizing, dolaisoleuine, dolaproine, dolaphenine and dolavaline from readily available starting materials such as Z-(S,S)isoleucine, S-phenylalaline, S-phenylalaninol, S-prolinol, S-mandelate, and S-valine. The requisite amino acids have been combined using several peptide coupling procedures to create pharmaceutically pure dolastatin 10.
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-1144360-B1 优先权日:1999-01-22 标题 :A method for the synthesis of compounds of formula 1 and derivatives thereof
专利号:CN-117623988-A 优先权日:2022-08-17 标题 :A kind of synthesis method of N-Boc-L-phenylalanin aldehyde
专利号:CN-116730873-A 优先权日:2022-03-02 标 题 :A kind of synthesis method of N-Boc-L-phenylalanin aldehyde
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
摘要:Okamoto, K.; Ohe, K., Science of Synthesis Knowledge Updates, (2020) 1, 77. 摘要:Ayad, T.; Pirat, J.-L.; Virieux, D., Science of Synthesis Knowledge Updates, (2022) 1, 321. 摘要:Dornan, L. M.; Hughes, N. L.; Muldoon, M. J., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 537. 摘要:Metternich, J. B.; Mudd, R. J.; Gilmour, R., Science of Synthesis: Photocatalysis in Organic Synthesis, (2017) 1, 394.