专利号:US-6815214-B2 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of diketopiperazines 发明人:BOYCE JIM P; HOWBERT J JEFFRY; TABONE JOHN C 权利人:CELLTECH R & D INC 摘要:The synthesis of novel diketopiperazines, their use in inhibiting cellular events such as those involving NFK-α, NFK-β and in the treatment of inflammation events, a combinatorial library of diverse diketopiperazines and process for their synthesis as a library and as individual compounds. In particular novel diketopiperazines are disclosed including their synthesis and use in cellular events such as activation of the transcription factor, nuclear factor, TNF-α, TNF-β and also apoptosis.
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-2007179279-A1 优先权日:2005-12-30 标题:Methods for the synthesis of arginine-containing peptides 发明人:CHEN LIN; ROBERTS CHRISTOPHER R 权利人:CHEN LIN; ROBERTS CHRISTOPHER R 摘要:Methods for the synthesis of arginine-containing peptides are provided. The methods include a step that minimizes contact of side chain protected arginine with base prior to the coupling step.
专利号:US-7122628-B2 优先权日:2000-12-22 标 题:Process for the synthesis of a peptide having a Trp residue 发明人:JACKSON STEVEN ALLEN 权利人:IPSEN MFG IRELAND LTD 摘要:A process for the solid phase synthesis of a peptide having at least one thyptophan residue, wherein said method comprises temporarily protecting the indole ring of said tryptophan residue with a side chain protecting group which is labile to a base wherein said protecting group is removed during cleavage of said peptide from the solid support.
专利号:US-12378196-B2 优先权日:2018-12-11 标 题 :Synthesis of (S)-6-hydroxytryptophan and derivatives thereof 发明人:SIMON WERNER; WERNER-SIMON SUSANNE; MüLLER CHRISTOPH 权利人:HEIDELBERG PHARMA RES GMBH 摘要:The present invention relates to novel methods and compounds for synthesizing amanitin derivatives. The invention in particular relates to methods for synthesizing (S)-6-hydroxy-tryptophan derivatives which can be used as building blocks for synthesizing amanitin derivatives or amatoxin drug conjugates. The invention further relates to intermediate compounds of said synthesis pathways for use in amanitin derivative and amatoxin drug conjugate synthesis, and to the use of particular catalysts suited for mediating said synthesis pathways.
专利号:US-3790555-A 优先权日:1972-01-20 标 题:Octapeptide derivative of gonadotropinreleasing hormone 发明人:FLOURET G; COLE J 权利人:ABBOTT LAB 摘要:THE SYNTHESIS OF THE OCTAPEPTIDE TRP-SER-TYR-GLY-LEUARG-PRO-GLY-AMIDE CARRYING EASILY REMOVABLE PROTECTIVE GROUPS ON THE SER, TYR, ARG AND TRP MOIETIES IS DESCRIBED. THE NEW SYNTHESIS USES AS THE STARTING MATERIAL TWO TETRAPEPTIDE FRAGMENTS CARRYING EASILY REMOVABLE PROTECTIVE GROUPS. ONE OF THESE FRAGMENTS, TRP-SER-TYR-GLY-OH WITH SUITABLE PROTECTIVE GROUPS, ALSO IS A PART OF THE PRESENT INVENTION. AFTER COUPLING OF THE TWO FRAGMENTS, THE PROTECTIVE GROUP ON THE AMINO-N OF THE TRYPTOPHANE MOIETY IS REMOVED TO OBTAIN AN OCTAPEPTIDE CARRYING EASILY REMOVABLE PROTECTIVE GROUPS WHICH CAN BE RETAINED VHILE BULIDING UP THE MOLECULE TO THE DECAPEPTIDE CHAIN WHICH IS THE GONADOTROPIN-RELEASING HORMONE, AFTER REMOVAL OF THESE PROTECTIVE GROUPS.
参考标题:5-Norbornene-2,3-Dicarboximido Carbonochloridate. A New Stable Reagent For The Introduction Of Amino-Protecting Groups 作者:Peter Henklein,Hans-Ulrich Heyne,Wolf-Rainer Halatsch,Hartmut Niedrich 摘要:The Synthesis Of Activated Carbonates, Based On A New Carbonochloridate Derived From N-Hydroxy-5-Norbornene-2,3-Dicarboximide, Is Reported. These Activated Carbonic Esters Are Excellent Reagents For The Introduction Of All Currently Used Urethane Protecting Groups.
合成参考文献
摘要:Wessjohann, L. A.; Kaluđerović, G. N.; Neves Filho, R. A. W.; Morejon, M. C.; Lemanski, G.; Ziegler, T., Science of Synthesis: Multicomponent Reactions, (2013) 1, 495. 摘要:Kroon, E.; Zarganes Tzitzikas, T.; Neochoritis, C. G.; Dömling, A., Science of Synthesis: Applications of Domino Transformations in Organic Synthesis, (2015) 2, 428. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025). 摘要:Leclerc, E., Science of Synthesis: Knowledge Updates, (2024) 3, 243. 参考文献:10.1063/1.2216696 摘要:Mitchell SA. Origin of second harmonic generation optical activity of a tryptophan derivative at the air/water interface. J Chem Phys. 2006 Jul 28;125(4):44716. doi: 10.1063/1.2216696.