17288-15-2Relevant articles and documents
Microwave-Assisted Ruthenium- and Rhodium-Catalyzed Couplings of α-Amino Acid Ester-Derived Phosphinamides with Alkynes
Li, Xue-Hong,Gong, Jun-Fang,Song, Mao-Ping
supporting information, (2021/12/23)
Two different types of new phosphinamide α-amino ester derivatives have been prepared in moderate to high yields via ruthenium(II) and rhodium(III)-catalyzed ortho-C?H functionalization under microwave irradiation. Specifically, the ortho-alkenylated phosphinamides were produced through coupling of phosphinamides containing an α-substituted or α,α-disubstituted α-amino ester with internal alkynes under ruthenium catalysis. In contrast, Ru and the more effective Rh-catalyzed coupling of the α-unsubstituted glycine ester phosphinamide with alkynes resulted in formation of oxidative annulation products, phosphaisoquinolin-1-ones. The developed methods feature the use of easily accessible starting materials, short reaction time, exclusive E-stereoselectivity (for ortho-alkenylation) and good functional group tolerance. The alkenylation reaction was readily scaled up to gram scale. Furthermore, the obtained alkenylated phosphinamide could be transformed into P-containing dipeptides through hydrolysis of the ester group in the catalysis product and subsequent condensation with an α-amino ester.
ANTIVIRAL PRODRUGS OF TENOFOVIR
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Page/Page column 29; 30; 33, (2018/09/26)
Compounds of Formula I: and pharmaceutically acceptable salts and co-crystals thereof are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
METHODS FOR TREATING ARENAVIRIDAE AND CORONAVIRIDAE VIRUS INFECTIONS
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Paragraph 0638-0639, (2017/04/04)
Provided are methods for treating Arenaviridae and Coronaviridae virus infections by administering nucleosides and prodrugs thereof, of Formula I: wherein the 1′ position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Lassa virus and Junin virus infections.
New Amino-Acid-Based β-Phosphorylated Nitroxides for Probing Acidic pH in Biological Systems by EPR Spectroscopy
Thétiot-Laurent, Sophie,Gosset, Ga?lle,Clément, Jean-Louis,Cassien, Mathieu,Mercier, Anne,Siri, Didier,Gaudel-Siri, Anouk,Rockenbauer, Antal,Culcasi, Marcel,Pietri, Sylvia
, p. 300 - 315 (2017/02/15)
There is increasing interest in measuring pH in biological samples by using nitroxides with pH-dependent electron paramagnetic resonance (EPR) spectra. Aiming to improve the spectral sensitivity (ΔaX) of these probes (i.e., the difference between the EPR hyperfine splitting (hfs) in their protonated and unprotonated forms), we characterized a series of novel linear α-carboxy, α′-diethoxyphosphoryl nitroxides constructed on an amino acid core and featuring an (α or α′)-C?H bond. In buffer, the three main hfs (aN, aH, and aP) of their EPR spectra vary reversibly with pH and, from aP or aH titration curves, a two- to fourfold increase in sensitivity was achieved compared to reference imidazoline or imidazolidine nitroxides. The crystallized carboxylate 10 b (pKa ≈3.6), which demonstrated low cytotoxicity and good resistance to bioreduction, was applied to probe stomach acidity in rats. The results pave the way to a novel generation of highly sensitive EPR pH markers.
METHODS FOR TREATING FILOVIRIDAE VIRUS INFECTIONS
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Paragraph 0236, (2016/05/19)
Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae vims infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula (IV): The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
PROCESS FOR THE PREPARATION OF ANAGRELIDE AND ANALOGUES THEREOF
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Paragraph 0094; 0095, (2013/08/28)
The present invention relates to a novel process for producing anagrelide, 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin 2(3H)-one, or certain analogues thereof. The process of the invention also provides improved processes for producing key intermedia
PROCESS FOR THE PREPARATION OF ANAGRELIDE AND ANALOGUES THEREOF
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Page/Page column 23-24; 30-31, (2012/05/05)
The present invention relates to a novel process for producing anagrelide, 6,7-dichloro-1,5- dihydroimidazo [2,1-b] quinazolin 2 (3H)-one, or certain analogues thereof. The process of the invention also provides improved processes for producing key interm
Antiviral phosphoramidates
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Page/Page column 18; 22, (2008/06/13)
The invention provides novel nucleoside compounds of formula I wherein R1, R2a, R2b, R3, R4, R5, R6, R8a, R9 and R10 are as defined herein which are useful for the treatment of Hepatitis C Virus (HCV) mediated diseases. The invention further provides methods for treatment or prophylaxis of HCV mediated diseases with compounds of formula I and pharmaceutical compositions comprising these compounds,
Microwave-assisted, zinc-mediated peptide coupling of N-benzyl-α,α-disubstituted amino acids
Cianci, Julia,Baell, Jonathan B.,Harvey, Andrew J.
, p. 5973 - 5975 (2008/02/10)
Incorporation of the extremely hindered amino acid N-benzylaminoisobutyric acid into dipeptides under microwave irradiation with commercial zinc dust is described. A comparative survey of various methodologies for hindered peptide couplings was undertaken
CHEMICAL COMPOUNDS
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Page/Page column 22, (2010/02/10)
Phosphoramidate derivatives of nucleotides and their use in the treatment of cancer are described. The base moieties of, for example, each of deoxyuridine, cytarabine, gemcitabine and citidine may be substituted at the 5-position. The phosphoramidate moiety has attached to the P atom an aryl-O moiety and an α-amino acid moiety. The α-amino acid moiety may correspond to or be derived from either a naturally occurring or a non-naturally occurring amino acid.