专利号:US-2021130409-A1 优先权日:2017-09-01 标 题 :Method for the Solid-Phase Synthesis of Cyclic Pentapeptides 发明人:ZHENGGUO JIANG; LUCIANO FORNI; ROBERTSON ALAN 权利人:Alsonex Pty Ltd 摘要:A method for the synthesis of a cyclic ornithine-proline-D-cyclohexylalanine-tryptophan-arginine pentapeptide of Formula A; n n n n n n n n n n n n wherein R 1 and R 2 are, independently, —H, or —C(O)R 3 where R 3 is —CH 2 Ph, —CH 2 CH 2 Ph, —CHâ•?CHPh, —C(NHAC)CH 2 Ph;n nthe method comprising the steps of;n nforming a linear proline-D-cyclohexylalanine-tryptophan-arginine-ornithine pentapeptide of Formula B, attached to a polymeric resin;n n n n n n n n n n n n n n n n n wherein R 1 is as for Formula A, RES indicates the polymeric resin, and P 1 and P 2 are protecting groups;n ncyclising the linear pentapeptide of Formula B to form a cyclic pentapeptide of Formula C, attached to the polymeric resin;n n n n n n n n n n n n n n n cleaving the cyclic peptide of Formula C from the resin providing a cleaved cyclic pentapeptide having a free amine group of an ornithine residue;n noptionally substituting the free amine group of the ornithine residue of the cleaved cyclic peptide;n nremoving the protecting groups P 1 and P 2 , to providethe cyclic peptide of Formula A.
专利号:US-2025059440-A1 优先权日:2023-08-14 标 题 :Synthesis of chalcogenide perovskite nanoparticles 发明人:HAGES CHARLES J; JESS ALEXANDER D; YANG RUIQUAN 权利人:UNIV FLORIDA 摘要:Disclosed herein are methods to synthesize perovskite nanoparticles in solution and at a relatively low temperature (110-300 C). This synthesis of low-temperature, solution-based chalcogenide perovskites were shown to produce materials with excellent optoelectronic properties. Furthermore, disclosed is a technique to stabilize the desired phase of these perovskites (particularly those phases which can not be fabricated in existing techniques). In addition, the material of the composition BaZrS3 (barium zirconium sulfide) has been synthesized in the perovskite crystal structure as nanoparticles for the first time.
专利号:US-11059835-B2 优先权日:2014-08-15 标 题 :Synthesis of cephalosporin compounds 发明人:WALLER DAVID; GAZDA GREGORY; MINDEN ZACHARY; BARTON LISA; LEIGH CLIFTON 权利人:MERCK SHARP & DOHME 摘要:Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.
专利号:WO-2025088147-A1 优先权日:2023-10-27 标题 :Theranostic psma-targeting ligands for the diagnosis and treatment of psma-expressing cancers and their solid phase synthesis 发明人:Schäfer Martin; BAUDER-WUEST ULRIKE; ROSCHER MAREIKE; REMDE YVONNE; BENEÅ OVÃ?-SCHÄFER MARTINA; BARINKA CYRIL; KUTILOVÃ? ZSÓFIA; MOTLOVÃ? LUCIA 权利人:DEUTSCHES KREBSFORSCHUNGSZENTRUM STIFTUNG DES OEFFENTLICHEN RECHTS 摘要:The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and radiopharmaceuticals for the treatment of various disease states of PSMA-expressing cancers, especially prostate cancer, and metastases thereof. Further the present invention provides synthetic procedures for the synthesis of such PSMA-targeting ligands.
专利号:WO-2024165749-A1 优先权日:2023-02-10 标 题:Synthesis of a water-based p-type donor polymer 发明人:FABIANO SIMONE; YANG CHI-YUAN; LIU TIEFENG; KROON RENEE; HEIMONEN JOHANNA 权利人:N INK AB 摘要:The present invention relates to a method for synthesizing a polymer comprising at least one repeating unit comprising at least one diaromatic moiety, at least one glycol side chain functionalized with a terminal carboxylate and/or sulfonate group, the method comprising the steps of: a) providing a glycol having general formula: H-(O-CH2-(CH2)m)n-OH wherein n is an integer from 1 to 50; and wherein m is an integer from 0 to 10; b) allowing the glycol to react with an aryl halide in presence of a copper halide catalyst, thus forming a first intermediate comprising a first aromatic moiety; c) allowing the first intermediate to undergo oxa-Michael addition to a Michael acceptor comprising a carboxylate and/or sulfonate precursor thus forming a second intermediate comprising the first aromatic moiety and one of the carboxylate and/or sulfonate precursor; d) brominating the first aromatic moiety of the second intermediate, thus forming a third intermediate comprising a brominated first aromatic moiety; e) allowing the brominated first aromatic moiety of the third intermediate to undergo a coupling reaction with a compound comprising a second aromatic moiety, thus forming a polymeric compound comprising at least one repeating unit comprising at least one diaromatic moiety, at least one glycol moiety with a terminal end comprising carboxylate and/or sulfonate precursor; f) deprotecting the carboxylate and/or sulfonate precursor thus forming a polymer comprising at least one repeating unit comprising at least one diaromatic moiety and at least one glycol side chain functionalized with a terminal carboxylate and/or sulfonate group.
专利号:US-2023046065-A1 优先权日:2019-11-25 标题 :MERGING C(sp3)-H ACTIVATION WITH DNA-ENCODING 发明人:YU JIN-QUAN 权利人:SCRIPPS RESEARCH INST 摘要:Palladium-catalyzed C(sp3)—H arylation of aliphatic carboxylic acids, amides and ketones with BNA-encoded aryl iodides in water is disclosed, Furthermore, sequential C—H arylation chemistry enabled the on-DNA synthesis of structurally-diverse scaffolds containing enriched C(sp3) character, chiral centers, cyclopropane, cyclobutane, and heterocycles. That new chemistry permits preparation of a DNA—encoded library (BEL) technology that can dramatically expedite hit identification in drug discovery owing to its ability to perform protein affinity selection with millions or billions of molecules in a single experiment. The sequential functionalization of multiple C—H bonds provides an unique avenue for creating diversity and complexity from simple starting materials. The use of water as solvent, the presence of DMA, and the extremely low concentration of DMA-encoded coupling partners (0.001 M) have previously hampered the development DMA-encoded C(sp3)—H activation reactions, but many of those hurdles have now been overcome.
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合成参考文献
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