专利号:WO-2012047907-A9 优先权日:2010-10-04 标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto 发明人:MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.
专利号:WO-2024182268-A1 优先权日:2023-02-27 标 题 :Liquid phase peptide support synthesis of peptides and peptidomimetics 发明人:HAN AMY 权利人:REGENERON PHARMA 摘要:The present invention provides compounds useful as support for liquid phase organic synthesis e.g., liquid phase organic synthesis of peptides and peptidomimetics. In one aspect, the present invention provides a compound having a structure of Formula (I) where R1, R2, R3, m, and n are as described herein and methods of making and using same.
专利号:EP-1473330-B1 优先权日:1996-07-17 标题:Process for the synthesis of oxonol compound 发明人:NISHIGAKI JUNJI; DEGUCHI YASUAKI 权利人:FUJI PHOTO FILM CO LTD 摘要:An oxonol compound is represented by the following formula (I): in which each of Z, W<1> and W<2> independently is an atomic group that forms a heterocyclic ring; and M is a cation. A process for the synthesis of an oxonol compound is disclosed.
专利号:US-11186608-B2 优先权日:2017-12-21 标 题 :Solid phase synthesis of acylated peptides 发明人:SCHOENLEBER RALPH O; LOIDL GUENTHER 权利人:BACHEM HOLDING AG 摘要:The present invention relates to methods and compounds for the solid phase synthesis of peptides carrying a substituent at an amino group of an amino acid side chain.
专利号:US-6632942-B2 优先权日:2000-05-04 标题:Asymmetric synthesis of piperazic acid and derivatives thereof 发明人:ROBIDOUX ANDREA L C; SERAFINI SIRO; DIETERICH PETRA; LEONARDI STEFANIA; STIBBARD JOHN 权利人:VERTEX PHARMA 摘要:This invention provides a concise, asymmetric synthesis of piperazic acid and derivatives thereof, whereby either the (3S)- or (3R)-enantiomeric form may be obtained with high optical purity. (3S)-piperazic acid is derived from D-glutamic acid through an (R)-2,5-dihydroxyvalerate ester intermediate. After the hydroxy groups are converted to suitable leaving groups, such as mesylates, the ester is treated with a bis-protected hydrazine to provide the desired (3S)-piperazic acid derivative. The (3R) enantiomer of piperazic acid may be similarly obtained starting with L-glutamic acid. The method may also be used to obtain piperazic acid derivatives that have moderate optical purity or are racemic. By this method, piperazic acid derivatives may be obtained that are useful as intermediates for pharmacologically active compounds. For example, certain intermediates of this invention are useful for preparing caspase inhibitors, particularly inhibitors of ICE, through additional steps known in the art.
专利号:WO-9915510-A1 优先权日:1997-09-24 标 题:Protecting and linking groups for organic synthesis 发明人:TOTH ISTVAN; DEKANY GYULA; KELLAM BARRY 权利人:ALCHEMIA PTY LTD; TOTH ISTVAN; DEKANY GYULA; KELLAM BARRY 摘要:This invention relates to methods for synthesis of organic compounds, and in particular to compounds useful as protecting and linking groups for use in the synthesis of peptides, oligosaccharides, glycopeptides and glycolipids. The invention provides protecting and linking groups which are useful in both solid phase and solution synthesis, and are particularly applicable to combinatorial synthesis. In its most general aspect, the invention provides a cyclic compound of general formula (I).
摘要:Barsegyan, Y. A.; Vil’, V. A.; Tomkinson, N. C. O.; Terent’ev, A. O., Science of Synthesis Knowledge Updates, (2022) 1, 260. 摘要:Ayad, T.; Pirat, J.-L.; Virieux, D., Science of Synthesis Knowledge Updates, (2022) 1, 293. 摘要:Ochoa, C. I.; Tambar, U. K., Science of Synthesis Knowledge Updates, (2020) 2, 363. 摘要:Shaabani, A.; Sarvary, A.; Shaabani, S., Science of Synthesis: Multicomponent Reactions, (2013) 2, 103. 摘要:Elliott, M. C.; Jones, D. H., Science of Synthesis: Multicomponent Reactions, (2013) 2, 280.