专利号:US-4965343-A 优先权日:1988-01-28 标题 :Method of peptide synthesis 发明人:FELIX ARTHUR M; FOURNIER ALAIN; DANHO WALEED 权利人:HOFFMANN LA ROCHE 摘要:A method for the solid phase synthesis of multi-sulfated peptides comprising coupling side-chain unprotected hydroxyamino acids to the peptide chain utilizing benzotriazol-1-yl-oxy-tris (dimethyl)-phosphonium hexafluorophosphate (BOP) as a coupling reagent.
专利号:US-7038037-B2 优先权日:2002-06-20 标题 :Method for sequential support-bound synthesis of conjugated oligomeric compounds 发明人:MAIER MARTIN A; GUZAEV ANDREI P; MANOHARAN MUTHIAH 权利人:ISIS PHARMACEUTICALS INC 摘要:A sequential support-bound synthesis method is disclosed for preparing a conjugated oligomeric compound, preferably a PNA-peptide conjugate or an oligonucleotide-peptide conjugate, using a bridging molecule having at least two N-protecting amino groups. A conjugated oligomeric compound for therapeutic or prophylactic delivery is also disclosed.
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:WO-2025052163-A1 优先权日:2023-09-07 标 题:2-amino-n-(benzo[d]thiazol-2-ylsulfonyl)-3-hydroxybutanamide derivatives acting as a threonyl-t-rna synthetase inhbitors for the treatment of malaria 发明人:JIRGENSONS AIGARS; BOLSAKOVA JEKATERINA; BOBROVS RAITIS; VARACEVA LARISA 权利人:LATVIAN INST ORGANIC SYNTHESIS 摘要:Representatives of 2-amino-N-(benzo[d]thiazol-2-ylsulfonyl)-3-hydroxybutanamide with general formula (I) show potency to inhibit malarial threonyl-tRNA synthetase (ThrRS) in low micromolar to nanomolar concentrations. As such they can be applied as compounds for prevention or treatment of malaria.
专利号:US-2004006203-A1 优先权日:2002-06-20 标题 :Method for sequential support-bound synthesis of conjugated oligomeric compounds
专利号:CN-113135979-A 优先权日:2020-01-18 标题 :A method for solid-phase synthesis of peptides
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144. [参考文献]: Antonio Procopio, Et Al. A Facile Er(Otf)3-Catalyzed Synthesis Of 2,3-Unsaturated O- And S-Glycosides. Carbohydr Res. 2007 Oct 15;342(14):2125-31.
合成参考文献
摘要:Sawamura, M.; Shimizu, Y., Science of Synthesis: Knowledge Updates, (2024) 2, 204.