专利号:EP-1586566-B9 优先权日:2004-03-29 标 题:P-toluenosulfonate salt of N-Methyl-N-(3,5-dimathoxy-2,4,6-triazinyl-1-)-morpholine and related compounds for use as condensing reagent in peptide synthesis 发明人:KAMINSKI ZBIGNIEW; KOLESINSKA BEATA; KOLESINSKA JUSTYNA; JASTRZABEK KONRAD 权利人:POLITECHNIKA LODZKA; KAMINSKI ZBIGNIEW; KOLESINSKA BEATA 摘要:The invention refers to new quarternary N-(3,5-disubstituted-1,3,5-triazinyl-1)-ammonium salts of sulfonic acids, with formula 1, where R1 and R2 denote in total or independently a halogen atom, an alkyl group, a substituted alkyl group, an alkoxy group, a substituted alkoxy group, a cycloalcoxy group, a substituted cycloalkoxy group, an aryl group, a substituted aryl group, an aryloxy group, a substituted aryloxy group, a heterocyclic group or a substituted heterocyclic group, preferably the methoxy group, where R3, R4, R5 denote independently each other an alkyl group, a substituted alkyl group, a cycloalkyl group, a substituted cycloalkyl group, an aryl group, a substituted aryl group, a heterocyclic or a substituted heterocyclic group, or form a heterocyclic ring with nitrogen atom, whereas O-SO2R6 denotes a sulfate anion, hydrosulfonate anion, arylsulfonate anion, preferable benzenosulfonate anion, p-toluenosulfonate anion, p-bromobenzenosulfonate anion, p-chlorobenzenosulfonate anion, alkylosulfonate anion, preferable methanosulfonate and trifluoromethanesulfonate anions or amidosulfonate anion. ?>The new compounds are designed for application as condensing reagents in syntheses of amides, esters, carboxylic acid hydroxides, and particularly in synthesis of peptides and their esters.
专利号:US-10544186-B2 优先权日:2016-11-09 标题:Process for the synthesis of amide bonds with the aid of novel catalysts 发明人:IGNATYEV NIKOLAI MYKOLA; FRANK WALTER; BARTHEN PETER; VYSOTSKY MYROSLAV 权利人:MERCK PATENT GMBH 摘要:The invention relates to a process for the production of amide bonds, in particular peptide bonds, with the aid of novel amide linking reagents containing an anion of the formula (I), to the novel reagents, and to the preparation thereof.
专利号:US-8471006-B2 优先权日:2003-10-31 标题:Coupling agents for peptide synthesis 发明人:CARPINO LOUIS A; XIA JUSONG; ZHANG CHONGWU; SFERDEAN CALIN DAN 权利人:CARPINO LOUIS A; XIA JUSONG; ZHANG CHONGWU; SFERDEAN CALIN DAN; UNIV MASSACHUSETTS 摘要:The present invention is directed to compounds of the formula: n nor salts thereof or N-oxides and their use in peptide synthesis.
专利号:US-2019270768-A1 优先权日:2016-11-09 标题 :Process for the synthesis of amide bonds with the aid of novel catalysts
专利号:US-9217012-B2 优先权日:2009-04-08 标题 :Inhibitors of protein tyrosine phosphatases 发明人:ZHANG ZHONG-YIN; ZHANG SHENG 权利人:ZHANG ZHONG-YIN; ZHANG SHENG; UNIV INDIANA RES & TECH CORP 摘要:Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.
专利号:US-4503040-A 优先权日:1984-02-27 标题:6-(Aminoacyloxymethyl)penicillanic acid 1,1-dioxides as beta-lactamase inhibitors 发明人:BARTH WAYNE E 权利人:PFIZER 摘要:Beta-lactamase inhibitors which are aminoacid esters of 6-alpha- and 6-beta-(hydroxymethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, said compositions useful in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoacyloxymethyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also useful in the treatment of bacterial infections; and intermediates therefor.
参考标题:α-N-Protected Dipeptide Acids: A Simple And Efficient Synthesis Via The Easily Accessible Mixed Anhydride Method Using Free Amino Acids In Dmso And Tetrabutylammonium Hydroxide 作者:G. Verardo,A. Gorassini |发布日期:2013.5 摘要:To Find Simple And Efficient Methods For Their Synthesis. For This Reason, We Have Investigated The Synthesis Of α‐n‐protected Dipeptide Acids By Reacting The Easily Accessible Mixed Anhydride Of α‐n‐protected Amino Acids With Free Amino Acids Under Different Reaction Conditions. The Combination Of Tba‐oh And Dmso Has Been Found To Be The Best To Overcome The Low Solubility Of Amino Acids In Organic
合成参考文献
参考文献:10.1007/s00726-011-0947-6 摘要:Islam MS, Bhuiyan MP, Islam MN, Nsiama TK, Oishi N, Kato T, Nishino N, Ito A, Yoshida M. Evaluation of functional groups on amino acids in cyclic tetrapeptides in histone deacetylase inhibition. Amino Acids. 2012 Jun;42(6):2103–10. doi: 10.1007/s00726-011-0947-6.