📜(2R)-2-Amino-2-Deutero-3-Hydroxypropanoic Acid置于sulfur Tetrafluoride,氢氟酸体系中,化学反应 3.0H,以80%的收率获得氟氘丙氨酸 参考文献:Synthesis Of (R)-Serine-2-D And Its Conversion To The Broad-Spectrum Antibiotic Fludalanine 标题:Synthesis Of (R)-Serine-2-D And Its Conversion To The Broad-Spectrum Antibiotic Fludalanine 摘要: Doi:10.1021/jo00391A029
专利号:US-3972921-A 优先权日:1974-11-08 标 题 :Synthesis of racemic 2-deutero-3-fluoro-alanine and its salts 发明人:DOLLING ULF-H; GRABOWSKI EDWARD J J; SCHOENEWALDT ERWIN F; SLETZINGER MEYER 权利人:MERCK & CO INC 摘要:The racemates of 2-deutero-3-fluoro-alanine and its salts are prepared by reductive amination of 3-fluoro-pyruvic acid, its hydrate or salts thereof, via the intermediate 2-imino-3-fluoro propionic acid salt, using alkali metal borodeuterides as reducing agents. The racemates thus obtained are valuable in the production of the corresponding 2-deutero-3-fluoro-D-alanine, and its pharmacologically acceptable salts, and derivatives thereof, which are potent antibacterial agents.
专利号:US-9693999-B2 优先权日:2011-01-26 标题:Small molecule RNase inhibitors and methods of use 发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE 权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education 摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.
专利号:US-5214130-A 优先权日:1990-02-27 标题 :Synthesis of novel immunosuppressive cyclosporin analogs with modified amino acids at position-8 发明人:PATCHETT ARTHUR A; TAUB DAVID; GOEGELMAN ROBERT T 权利人:MERCK & CO INC 摘要:New immunosuppressive cyclosporin analogs are disclosed consisting of [dehydro-Ala]8 cyclosporins and derived therefrom cyclosporins having a sulfur containing amino acid at position-8.
专利号:WO-2009056955-A1 优先权日:2007-10-30 标题 :Amine-bearing phospholipids (abps), their synthesis and use 发明人:ZUMBUEHL ANDREAS 权利人:UNIV BASEL; ZUMBUEHL ANDREAS 摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.
专利号:US-9868747-B2 优先权日:2014-02-18 标题:Marinopyrrole derivatives and methods of making and using same 发明人:LI RONGSHI; SEBTI SAID; LIU YAN; QIN YONG; SONG HAO; CHENG CHUNWEI 权利人:H LEE MOFFITT CANCER CT & RES; CHONGQING ZEIN PHARMACEUTICAL CO LTD 摘要:Marinopyrrole derivatives and methods for their synthesis and use are described herein. Novel cyclic and symmetric marinopyrroles with triazole substituents having antibacterial activity against resistant bacterial strains, such as MRSA are introduced. Also provided are methods of using the compounds for treating or preventing cancer and/or microbial infections.
专利号:US-9907753-B2 优先权日:2010-03-19 标 题 :Lipid vesicle compositions and methods of use 发明人:IRVINE DARRELL J; MOON JAEHYUN 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The invention provides delivery systems comprised of stabilized multilamellar vesicles, as well as compositions, methods of synthesis, and methods of use thereof. The stabilized multilamellar vesicles may comprise prophylactic, therapeutic and/or diagnostic agents.
1: Musson DG, Maglietto SM, Hwang SS, Gravellese D, Bayne WF. Simultaneous quantification of cycloserine and its prodrug acetylacetonylcycloserine in plasma and urine by high-performance liquid chromatography using ultraviolet absorbance and fluorescence after post-column derivatization. J Chromatogr. 1987 Feb 20;414(1):121-9. 6: Esposito AL, Pennington JE. Experimental pneumonia due to Haemophilus influenzae: observations on pathogenesis and treatment. J Infect Dis. 1984 May;149(5):728-34.
合成参考文献
参考文献:10.1007/s00044-023-03103-0 摘要:Renault YJG, Diao J, Cordes DB, Leach K, O’Hagan D. Direct syntheses of stereoisomers of 3-fluoro GABA and β-fluoroamine analogues of the calcium receptor (CaR) agonists, cinacalcet, tecalcet, fendiline and NPS R-467. Med Chem Res. 2023 Jul;32(7):1532–42. doi: 10.1007/s00044-023-03103-0.