CAS: 856866-72-3; (R)-3-(3-Fluoro-4-(6-(2-Methyl-2H-Tetrazol-5-yl)Pyridin-3-yl)Phenyl)-5-(Hydroxymethyl)Oxazolidin-2-One

上下游产品

CAS号1220910-89-3 N-[3-氟-4-[6-(2-... | CAS号60456-26-0 (R)-(-)-缩水甘油丁酯 | CAS号624-28-2 2,5-二溴吡啶 | CAS号97483-77-7 5-溴-2-氰基吡啶

N-[3-氟-4-[6-(2-甲基-2H-四唑-5-基)-3-吡啶基]苯基]氨基甲酸苄酯置于n,N-二甲基丙烯基脲,叔丁基锂,(R)-(-)-丁酸缩水甘油酯体系中,用 四氢呋喃 作为反应溶剂,化学反应 15.0H,以95%的收率获得产物特地唑胺
参考文献:一种磷酸特地唑胺的制备方法
标题:一种磷酸特地唑胺的制备方法
摘要:本发明公开了一种磷酸特地唑胺的制备方法,具体包括:以n‑[3‑氟‑4‑[6‑(2‑甲基‑2H‑四唑‑5‑基)‑3‑吡啶基]苯基]氨基甲酸苄酯为起始原料,在r1‑o‑m,1,3‑二甲基‑3,4,5,6‑四氢‑2‑嘧啶酮存在下,与r‑缩水甘油丁酸酯反应,再用pocl3磷酸酯化得到磷酸特地唑胺粗品,用碱溶液调ph值为7~9将其转换为盐,再用盐酸调ph值至1~2得到精制品磷酸特地唑胺.本发明具有反应条件温和,成本较低,操作简便,副反应较少,收率高,反应重现性好,经济环保且适于工业化生产的优点.

专利信息

专利号:US-11485721-B2
优先权日:2017-11-21
标 题:Method for the metal-free preparation of a biaryl by a photosplicing reaction and their uses
发明人：KLOSS FLORIAN; NEUWIRTH TONI; HAENSCH VEIT; HERTWECK CHRISTIAN
权利人:LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST HKI; LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST
摘要:The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar—Ar′ by photochemically reacting a precursor compound of formula (II): Ar—L—Ar′ to form a biaryl compound of general formula: Ar—L—Ar′(II)→Ar—Ar′ (I) wherein Ar and Ar′, independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5-20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group —X—Y—Z— as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.

专利号:US-10443047-B2
优先权日:2014-05-01
标题 :Increasing cellular lipid production by increasing the activity of diacylglycerol acyltransferase and decreasing the activity of triacylglycerol lipase
发明人：TSAKRAKLIDES VASILIKI; BREVNOVA ELENA E
权利人:NOVOGY INC
摘要:Disclosed are methods and compositions for increasing the triacylglycerol content of a cell by up-regulating diacylglycerol acyltransferase and down-regulating triacylglycerol lipase. In some embodiments, a DGA1 protein is expressed and a native TGL3 gene is knocked out, thereby increasing the synthesis of triacylglycerol and decreasing its consumption, respectively.

专利号:US-2023364251-A1
优先权日:2020-08-06
标 题:Methods for the synthesis of protein-drug conjugates
发明人：BORCHARDT ALLEN; HUGHES ROBERT MICHAEL
权利人:CIDARA THERAPEUTICS INC
摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.

专利号:US-10472663-B2
优先权日:2015-01-21
标 题:Procedure for the rapid determination of bacterial susceptibility to antibiotics that inhibit protein synthesis
发明人：FERNÃ?NDEZ GARCÃ?A JOSÉ LUIS; GOSÃ?LVEZ BERENGUER JAIME; BOU ARÉVALO GERMÃ?N; TAMAYO NOVAS MARIA; SANTISO BRANDARIZ REBECA; OTERO FARIÑA FÃ?TIMA MARÃ?A
权利人:ABM TECH LLC
摘要:The present invention relates to a method for the rapid evaluation of bacterial susceptibility or non-susceptibility of bacteria to antibiotics that inhibit protein synthesis. The rationale is to identify bacterial responses that depend or are influenced by protein synthesis. If this response is prevented or reduced by the antibiotic that inhibits the protein synthesis, the bacteria are susceptible to this antibiotic. Otherwise, if the response keeps similar despite the incubation with the antibiotic, the bacteria are not susceptible or resistant to this antibiotic. These responses could be determined at the DNA lev-el, cell wall level, morphological level or any other experimental approach, including metabolic, bio-chemical, physiological or genetic processes.

专利号:US-8461188-B2
优先权日:2011-10-20
标题 :Therapeutic combination of daptomycin and protein synthesis inhibitor antibiotic, and methods of use
发明人：BARTIZAL KENNETH F; LOCKE JEFFREY B; SHAW KAREN JOY; PROKOCIMER PHILIPPE G
权利人:TRIUS THERAPEUTICS INC
摘要:A therapeutic combination comprises an antibacterially effective amount of daptomycin, and an amount of protein synthesis inhibitor antibiotic effective to prevent the development of daptomycin non-susceptibility in bacteria. Related combination therapies and methods are also included.

专利号:US-2024207302-A1
优先权日:2021-04-01
标 题 :Antiviral compounds, methods for the manufacturing of compounds, antiviral pharmaceutical composition, use of the compounds and method for the oral treatment of coronavirus infection and related diseases thereof
发明人：CALIXTO JOãO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO
权利人:CALIXTO JOAO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO
摘要:The present invention relates to antiviral compounds selected from cytokinins, their nucleosides and nucleotide analogs, and their prodrugs as inhibitors of viral RNA synthesis, or their salts, solvates, derivatives, or even combinations of aforementioned compounds, for prophylactic treatment, curative (therapeutic) or mitigative coronavirus infection, represented by human and veterinary coronavirus, SARS-COV-2 and MHIV, and for the treatment of individuals potentially exposed to COVID-19. The present invention also comprises the methods for the manufacturing of such compounds, the antiviral pharmaceutical composition containing the compounds of the invention, as well as the use of the compounds, combinations of compounds, and method for the prophylactic, curative (therapeutic) or mitigative treatment of coronavirus infection, represented by coronavirus, in especial SARS-COV-2 and of patients with COVID-19, individual infected with SARS-COV-2 or potentially exposed to this virus. The antiviral activity of the compounds of this invention against SARS-COV-2 was greatly enhanced by inhibiting the 3′-5′-exonuclease. Synergistic results of the compounds according to the present invention were obtained from the combination with repurposed drugs.