18226-16-9Relevant academic research and scientific papers
PYRIMIDINE COMPOUND, PREPARATION METHOD THEREOF AND MEDICAL USE THEREOF
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Paragraph 0359; 0672; 0673, (2021/04/10)
The present invention discloses a pyrimidine compound, a preparation method thereof and a medical use thereof. Specifically, the present invention discloses a pyrimidine compound represented by formula (I), pharmaceutically acceptable salts thereof, a preparation method thereof, and a use thereof as a cyclin-dependent kinase 9 (CDK9) inhibitor, particularly for the treatment of cancer. The definition of each group in formula (I) is the same as that in the specification.
HETEROCYCLIC COMPOUND AS SYK INHIBITOR AND/OR SYK-HDAC DUAL INHIBITOR
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Paragraph 0167-0168, (2019/10/29)
A heterocyclic compound as a Syk inhibitor and/or a Syk-HDAC dual inhibitor, or pharmaceutically acceptable salts, prodrugs, deuterated derivatives, hydrates, and solvates thereof. Specifically, the present invention relates to a compound of formula (I), the compound having dual inhibitory activity for Syk and/or Syk-HDAC.
A Direct C-H/Ar-H Coupling Approach to Oxindoles, Thio-oxindoles, 3,4-Dihydro-1 H-quinolin-2-ones, and 1,2,3,4-Tetrahydroquinolines
Hurst, Timothy E.,Gorman, Ryan M.,Drouhin, Pauline,Perry, Alexis,Taylor, Richard J. K.
supporting information, p. 14063 - 14073 (2016/02/18)
A copper(II)-catalysed approach to oxindoles, thio-oxindoles, 3,4-dihydro-1H-quinolin-2-ones, and 1,2,3,4-tetrahydroquinolines via formal C-H, Ar-H coupling is described. In a new variant, copper(II) 2-ethylhexanoate has been identified as an inexpensive and efficient catalyst for this transformation, which utilises atmospheric oxygen as the re-oxidant. Copper(II) 2-ethylhexanoate: The synthesis of oxindoles, thio-oxindoles, 3,4-dihydro-1H-quinolin-2-ones, and 1,2,3,4-tetrahydroquinolines from linear precursors by direct C-H, Ar-H coupling by using a single copper catalyst is reported (see scheme; DIPEA=diisopropylethylamine, EWG=electron-withdrawing group). The cyclisations are simple to perform, run open to the air, are moisture insensitive, and use an inexpensive catalyst.
Thermodynamics of binding between α- and β-cyclodextrins and some p-nitro-aniline derivatives: Reconsidering the enthalpy-entropy compensation effect
Meo, Paolo Lo,D'Anna, Francesca,Gruttadauria, Michelangelo,Riela, Serena,Noto, Renato
, p. 9099 - 9111 (2007/10/03)
The thermodynamics of binding between native α- and β-cyclodextrin towards several p-nitro-aniline derivatives was examined, in order to gain further insights about the occurrence of different interaction modes for the two hosts. Valuable information was
HEAVY-ATOM KINETIC ISOTOPE EFFECTS IN THE BASE-CATALYZED SMILES REARRANGEMENT OF N-METHYL-2-(4-NITROPHENOXY)ETHANAMINE
Yilmaz, Ibrahim,Shine, Henry J.
, p. 603 - 608 (2007/10/02)
Carbon (k12C/k13C), nitrogen (k14N/k15N), and oxygen (k16O/k18O) kinetic isotope effects (KIE) have been measured in the hydroxide ion-catalyzed rearrangement of N-methyl-2-(4-nitrophenoxy)ethanamine, 2, to N-(2-hydroxyethyl)-N-methyl-4-nitroaniline, 4.KIE were measured at ambient temperature and at 1E-3 and 1E-1 M hydroxide ion concentrations.For measuring carbon KIE, 2 was enriched at the 1-position of the ring with 13C, while for measuring oxygen KIE, the phenoxy oxygen atom was enriched with 18O.KIE were obtained from isotopic abundances in 4 measured with whole-molecule-ion, quadrupole mass spectrometry.For measuring nitrogen KIE, unenriched 2 was used, and 29N2/28N2 ratios in 4 were measured by isotope-ratio mass spectrometry.The KIE results are consistent with the mechanism reported by Knipe and co-workers.In this mechanism, the rate-limiting step changes from formation of a Meisenheimer complex at high to its deprotonation at low hydroxide ion concentration.Thus at 1E-3 M hydroxide ion concentration the carbon and nitrogen isotope effects measured were, in fact, equilibrium IE, while at 1E-1 M hydroxide ion concentration they were for the formation of the Meisenheimer complex.Oxygen KIE were close to unity, and are regarded as either negligible or attributable to secondary IE associated with changes in bond hybridization rather than bond breaking.
Effects of N-Alkyl Substitution on the Formation and Rate-limiting Deprotonation of the Spiro-Meisenheimer Intermediate of Smiles Rearrangement of 2-(p-Nitrophenoxy)ethylamine, in Aqueous Solution
Knipe, Anthony C.,Sridhar, Narayan,Lound-Keast, Joseph
, p. 1893 - 1900 (2007/10/02)
For intramolecular rearrangement of 2-(p-nitrophenoxy)ethylamines to the corresponding 2-(p-nitro-anilino)ethanols the kinetic effects of N-alkyl substitution have been interpreted in terms of a mechanism whereby base-independent formation of a spiro-Meisenheimer intermediate is rate determined at high base concentrations but general-base-catalysed deprotonation of the intermediate (β 0.18-0.35) becomes rate determining at low base concentration.Reactions of the N-ethyl and N-isopropyl substrates are further complicated by a change to a specific-base-catalysed mechanism in ethanolamine buffers of high concentration; this observation requires that formation of the product by ring opening of the anionic spiro-Meisenheimer intermediate is not sensitive to general-acid catalysis.
