73899-15-7Relevant articles and documents
Synthesis of an [125I]-labelled derivative of MK-571, a tool for LTD4 receptor studies
Li,Leblanc,Zamboni,Young
, p. 537 - 544 (1994)
An [125I]-labelled derivative of MK-571 2 was synthesized from the arylstanne derivative 11 in 50% radiochemical yield. Compound 2 is a useful tool for LTD4 receptor studies. The arylstanne intermediate 11 was obtained from the coupl
A silicon-labelled amino acid suitable for late-stage fluorination and unexpected oxidative cleavage reactions in the preparation of a key intermediate in the Strecker synthesis
Scroggie, Kymberley R.,Alcock, Lisa J.,Matos, Maria J.,Bernardes, Gon?alo J. L.,Perkins, Michael V.,Chalker, Justin M.
, (2018)
A novel silicon-substituted phenylalanine derivative was prepared using the Strecker amino acid synthesis. An unexpected oxidative cleavage was observed in the preparation of the aldehyde required for the Strecker reaction. In this step, a homobenzylic alcohol intermediate was oxidatively cleaved to the corresponding benzaldehyde using either chromium or palladium based oxidants. This undesired side reaction was overcome through the use of Dess-Martin Periodinane, or through an efficient TEMPO-bleach oxidation. The amino acid prepared in this study was then labelled with fluoride in aqueous solvent using a range of fluoride sources. The efficiency of this labelling motivates future studies in late-stage fluorination of peptide and protein therapeutics for use in positron emission tomography.
Synthesis of some nitroimidazole substituted boronic acids: Precursors to technetium-99m complexes with potential for imaging hypoxic tissue
Raju,Ramalingam,Nowotnik
, p. 10233 - 10238 (1992)
A number of nitroimidazole substituted alkyl and aryl-boronic acids were synthesized as precursors to technetium-99m complexes under investigation as potential imaging agents of hypoxia. Compounds were prepared with nitro group either in the 2- or 4-posit
ADENOSINE RECEPTOR BINDING COMPOUNDS
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Paragraph 00284; 00298; 00374, (2020/02/06)
The present invention relates to pharmaceutical compounds and compositions of Formula (I) and methods of treatment using the compounds and compositions, especially for the treatment and/or prevention of a proliferation disorder, such as cancer. Compounds of Formula (I) as further described herein are shown modulators of the adenosine A2A receptor and exhibit antiproliferative activity. Accordingly, these compounds are useful to treat proliferative disorders such as cancer, and other adenosine receptor-related conditions including an inflammatory disease, renal disease, diabetes, vascular disease, lung disease, or an autoimmune disease.
Nitroxide derivative of ROCK kinase inhibitor
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Paragraph 0357-0363, (2020/06/17)
The invention provides a small molecular compound of a NO donor. The small molecular compound is characterized in that the small molecular compound is a compound shown represented by structural formula I shown in the description, or a stereoisomer, a geometrical isomer, a tautomer, a racemate, a deuterated isotope derivative, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof; and in the formula I, ring A is a substituted or unsubstituted heteroaromatic ring, X is selected from (CH2)n, n is selected from 0, 1, 2 and 3, R is a substituent group of terminal -O-NO2, R is selected from hydrogen, a hydroxyl group, halogen, an amino group, a cyano group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group and a substituted or unsubstituted heteroalkyl group, and R and R are respectively and independently selected from hydrogen, a substituted or unsubstituted alkyl group, a substituted or unsubstituted naphthenic base or an amino protecting group, or R and R are connected to form a substituted or unsubstituted cyclic heteroalkyl group. The compound has a high-activity inhibition effect on ROCK kinase.
ANTIMICROBIAL COMPOUNDS AND METHODS
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Paragraph 00420; 00807, (2020/07/31)
The invention is directed to compounds that are active as antibacterial agents. The invention compounds are active against gram-positive and gram-negative bacteria and can be used to treat infections caused by gram-positive and gram-negative bacteria. Also disclosed are processes and intermediates for making the compounds.
ANTIMICROBIAL COMPOUNDS AND METHODS
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Paragraph 00360, (2020/07/31)
The invention is directed to compounds that are active as antibacterial agents. The invention compounds are active against gram-positive and gram-negative bacteria and can be used to treat infections caused by gram-positive and gram-negative bacteria. Also disclosed are processes and intermediates for making the compounds.
Preparation method of new anti-allergic medicine Bilastine intermediate
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Paragraph 0044; 0045, (2017/08/28)
The invention discloses a preparation method of a new anti-allergic medicine Bilastine intermediate. Quaternary carbon atoms difficult to construct are constructed by using a mild addition reaction, carboxylic groups are introduced at room temperature by
Synthesis and characterization of polytriphenylamine based graft polymers for photorefractive application
Cao, Zhenbo,Abe, Yosuke,Nagahama, Takuo,Tsuchiya, Kousuke,Ogino, Kenji
, p. 269 - 276 (2013/02/25)
Novel graft copolymers, PTPA-g-PEAs containing poly(triphenylamine) (PTPA) backbone and poly(ethyl acrylate) (PEA) branches were synthesized by the oxidative coupling polymerization of triarylamine monomers followed by grafting of ethyl acrylate via an at
A total synthesis of millingtonine a
Wegner, Jens,Ley, Steven V.,Kirschning, Andreas,Hansen, Anne-Lene,Montenegro Garcia, Javier,Baxendale, Ian R.
supporting information; experimental part, p. 696 - 699 (2012/04/17)
A total synthesis of millingtonine A, a diglycosylated alkaloid, has been accomplished. Millingtonine A possesses a unique racemic tricyclic core structure not known from any other natural or synthetic source until now. The synthesis features a key bond-f
