专利号:US-2025188022-A1 优先权日:2022-02-07 标 题 :Process for the preparation of nafamostat, camostat and their derivatives 发明人:AHMED RIYAZ; KUMAR GULSHAN; MAHAJAN SHEENA; Verma Praveen Kumar; CHAM PANKAJ SINGH; KUMAR AMIT; AHMED QAZI NAVEED; REDDY DUMBALA SRINIVASA; SHANKAR RAVI; SINGH PARVINDER PAL 权利人:COUNCIL SCIENT IND RES 摘要:The invention provides a novel, economical and practical route for the synthesis of an ester from acid and alcoholic functionalities using Trihalotriazine as coupling agent. Specifically, the invention provides a novel, economical and practical route for the preparation of Nafamostat and Camostat. Synthesis of p-guanidinobenzoic acid (Al) was also achieved from thiourea and p-aminobenzoic acid by using trihalotriazine as coupling reagent.
[参考文献]: F S Steven, Et Al. Evidence For An Enzyme Which Cleaves The Guanidinobenzoate Moiety From Active-Site Titrants Specifically Designed To Inhibit And Quantify Trypsin. Eur J Biochem. 1983 Feb 1;130(2):335-9. [参考文献]: G T Layton, Et Al. The Specificity Of Murine Polyclonal And Monoclonal Antibodies To The Haptenic Drug Chlorhexidine Induced By Chlorine-Generated Chlorhexidine-Protein Conjugates. Clin Exp Immunol. 1987 Jul;69(1):157-65. [参考文献]: H J Nolte, Et Al. Kinetics And Mechanism For The Conformational Transition In P-Guanidinobenzoate Bovine Trypsinogen Induced By The Isoleucine-Valine Dipeptide. Biophys Chem. 1979 Nov;10(3-4):253-60. [参考文献]: K Beckh, Et Al. Elimination Of The Low-Molecular Weight Proteinase Inhibitor Camostate (Foy 305) And Its Degradation Products By The Rat Liver. Res Exp Med (Berl). 1987;187(6):401-6. [参考文献]: K Beckh, Et Al. Hepatic And Pancreatic Metabolism And Biliary Excretion Of The Protease Inhibitor Camostat Mesilate. Int J Pancreatol. 1991 Nov-Dec;10(3-4):197-205.
合成参考文献
参考文献:10.1038/s41566-023-01180-6 摘要:Li F, Deng X, Shi Z, Wu S, Zeng Z, Wang D, Li Y, Qi F, Zhang Z, Yang Z, Jang S, Lin FR, Tsang S, Chen X, Jen AK-. Hydrogen-bond-bridged intermediate for perovskite solar cells with enhanced efficiency and stability. Nat. Photon. 2023 Apr 10;17(6):478–84. doi: 10.1038/s41566-023-01180-6. 参考文献:10.1038/s41578-024-00678-x 摘要:Jiang Q, Zhu K. Rapid advances enabling high-performance inverted perovskite solar cells. Nat Rev Mater. 2024 May 17;9(6):399–419. doi: 10.1038/s41578-024-00678-x. 参考文献:10.1038/s41566-024-01506-y 摘要:He Y, Song J, Li M, Sakhatskyi K, Li W, Feng X, Yang B, Kovalenko M, Wei H. Perovskite computed tomography imager and three-dimensional reconstruction. Nat. Photon. 2024 Aug 16;18(10):1052–8. doi: 10.1038/s41566-024-01506-y. 参考文献:10.1038/s44160-025-00896-3 摘要:Zhu P, Liu Z, Lei X, He S, Wang D, Zeng J, Wang L, Su F, Peng W, Liang Z, Sun Y, Lei Z, Li Z, Hsu H, Pan X, Wang X, Li J, Zhang Y, Xu B. Symmetry-driven engineering of long-range-ordered π–π stacking molecules for high-efficiency perovskite photovoltaics. Nat. Synth. 2025 Sep 30;5(1):64–73. doi: 10.1038/s44160-025-00896-3. 参考文献:10.1007/978-3-032-15441-5_27 摘要:Tripathi V, Mishra GR, Pratap J, Singh S. Recent Advancements in Perovskite Based Tandem Solar Cells. 2026. In: Springer Proceedings in Physics.