专利号:US-2018265547-A1 优先权日:2014-07-18 标 题 :Z-selective olefin metathesis of peptides 发明人:MANGOLD SHANE L; GRUBBS ROBERT H 权利人:CALIFORNIA INST OF TECHN 摘要:The invention relates generally to the synthesis of modified amino acids and modified peptides in the presence of cyclometalated catalysts. The invention has utility in the fields of catalysis, organic synthesis, polymer chemistry, and industrial and fine chemicals chemistry.
专利号:US-6841559-B1 优先权日:1999-11-19 标 题:Pyridinones to treat and prevent bacterial infections 发明人:ALMQVIST FREDERIC; EMTENAS HANS; HULTGREN SCOTT J; PINKNER JEROME S 权利人:WASHINGTON UNIVERSITY OF ST LO 摘要:Novel pyridinones and their derivatives which are effective in treating or preventing Gram-negative bacterial infections are provided. The pyridinones are stable and easily derivatized; the methods by which these derivatizations occur is described. Two regioselective and functional group tolerant methods for the synthesis of the novel pyridinones are also provided. One such synthetic method involves reacting an imine and a Meldrum's acid derivative in solution. The other synthetic method is a solid phase synthesis of the pyridinones in which an imine is prepared bound to a solid support and a Meldrum's acid derivative is reacted with the imine. Novel imine intermediates useful in the solid phase and solution methods of synthesizing the pyridionones are also described.
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-2011076718-A1 优先权日:2008-02-27 标题:In vivo incorporation of an unnatural amino acid comprising a 1,2-aminothiol group 发明人:FICHT SIMON; JAHNZ MICHAEL; GRUNEWALD JAN; SCHILLER STEFAN; SCHULTZ PETER G 权利人:SCRIPPS RESEARCH INST 摘要:The invention relates to orthogonal pairs of tRNAs and aminoacyl-tRNA synthetases that can incorporate unnatural amino acids that comprise a 1,2 aminothiol group into polypeptides. The invention provides translation systems in which polypeptides comprising unnatural amino acids that comprise a 1,2 aminothiol group can be produced. The invention also provides methods for producing polypeptides containing unnatural amino acids that comprise a 1,2 aminothiol group. Also provided by the invention are compositions comprising orthogonal aminoacyl-tRNA synthetases that preferentially aminoacylate a cognate orthogonal tRNA with unnatural amino acids that comprise a 1,2 aminothiol group. The invention provides methods for the synthesis of the unnatural amino acid 2-amino-3-(4-(2-amino-3-mercaptopropan-amido)phenyl)-propanoic acid.
专利号:US-3795666-A 优先权日:1969-08-01 标 题 :Method of synthesizing peptides in the presence of a carbodiimide and of 3-hydroxy-4-oxo-3,4-dihydro-1,2,3-benzotriazine 发明人:KONIG W; GEIGER R; WOLF E 权利人:HOECHST AG 摘要:IMPROVED SYNTHESIS OF PEPTIDES BY THE CARBODIIMIDE METHOD IN WHICH AN AMINO-PROTECTED AMINO ACID OR PEPTIDE HAVING A REACTIVE CARBOXY GROUP IS CONDENSED WITH A CARBOXY-PROTECTED AMINO ACID OR PEPTIDE HAVING A REACTIVE AMINO IN THE PRESENCE OF 3-HYDROXY-4-OXO3,4-DIHYDRO-1,2,3-BENZOTRIAZINE AS WELL AS IN THE PRESENCE OF A CARBODIIMIDE SUCH AS DICYCLOHEXYL CARBODIIMIDE.
专利号:US-11679168-B2 优先权日:2018-09-14 标 题 :Caspase-3-triggered molecular self-assembling PET probes and uses thereof 发明人:RAO JIANGHONG; CHENG YUNFENG; CHEN MIN; XIE JIANGHANG; CHEN ZIXIN 权利人:UNIV LELAND STANFORD JUNIOR; THE BOARD OF TRUSTEES OF LELAND STANFORD JUNIOR UNIV 摘要:Embodiments of the synthesis, radiolabeling and biological applications of an activatable tracer that undergoes intramolecular cyclization and aggregation upon activation by cleavage of a blocking moiety are provided. The probes of the disclosure allow for target-controlled self-assembly of small molecules in living subjects for imaging and drug delivery. The aggregated nanoprobes of the disclosure may be detectable optically, by PET detection, magnetic resonance imaging, and the like depending on the detectable reporter attached to the nanoprobe.
参考标题:Divergent Approach For The Synthesis Of Gombamide A And Derivatives 作者:Mohana Rao Vippila,Sameer Nikhar,Alan P. Gracia,Gregory D. Cuny |发布日期:2016.9.16 摘要:A Synthesis Of Gombamide A (1) Using N-Terminal Peptide Extension, Oxidative Disulfide Bond Formation, And Late-Stage 4-Hydroxystyrylamide Installation Has Been Achieved. This Divergent Method Was Also Utilized To Synthesize Several Gombamide A Derivatives With Modification To The 4-Hydroxystyrylamide Via Cyclic Peptide 2. The Natural Product And Four Derivatives Were Found To Be Devoid Of Na+/k+-Atpase
合成参考文献
参考文献:10.1055/s-0040-1705903 摘要:Depalmitoylation Strategy to Inhibit NRAS Signaling. Synfacts. 2020 Sep 17;16(10):1226. doi: 10.1055/s-0040-1705903. 参考文献:10.1007/978-1-4939-2272-7_5 摘要:Cui L, Rao J. 2-Cyanobenzothiazole (CBT) condensation for site-specific labeling of proteins at the terminal cysteine residues. Methods Mol Biol. 2015;1266():81–92. doi: 10.1007/978-1-4939-2272-7_5.