87488-61-7Relevant articles and documents
HETEROCYCLIC COMPOUNDS AS MODULATORS OF STIMULATOR OF INTERFERON GENES (STING)
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Page/Page column 101-102, (2021/06/22)
The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.
Conjugate Addition Routes to 2-Alkyl-2,3-dihydroquinolin-4(1H)-ones and 2-Alkyl-4-hydroxy-1,2-dihydroquinoline-3-carboxylates
Kingsbury, Alex,Brough, Steve,McCarthy, Antonio Pedrina,Lewis, William,Woodward, Simon
supporting information, p. 1011 - 1017 (2019/12/27)
Under CuBr·SMe2/PPh3 catalysis (5/10 mol-%) RMgCl (R = Me, Et, nPr, CH=CH2, nBu, iBu, nC5H11, cC6H11, Bn, CH2Bn, nC11H23) readily (–78 °C) undergo 1,4-addition to Cbz or Boc protected quinolin-4(1H)-ones to provide 2-alkyl-2,3-dihydroquinolin-4(1H)-ones (14 examples, 54–99 % yield). Asymmetric versions require AlEt3 to Boc-protected ethyl 6-substituted 4(1H)-quinolone-3-carboxylates (6-R group = all halogens, n/i/t-alkyls, CF3) and provide 61–91 % yield, 30–86 % ee; any halogen, Me, or CF3 provide the highest stereoselectivities (76–86 % ee). Additions of AlMe3 or Al(nC8H17)3 provide ≈ 45 and ≈ 75 % ee on addition to the parent (6-R = H). Ligand (S)-(BINOL)P–N(CHPh2)(cC6H11) provides the highest ee values engendering addition to the Si face of the 4(1H)-quinolone-3-carboxylate. Allylation and deprotection of a representative 1,4-addition product example confirm the facial selectivity (X-ray crystallography).
Pyrimidine compounds
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Paragraph 0029; 0032; 0033, (2017/09/08)
The present invention belongs to the field of pharmaceutical synthesis, and relates to pyrimidine compounds, a preparation method and applications thereof, a pharmaceutical composition containing the pyrimidine compounds as active components, and applications of the pyrimidine compounds in preparation of antitumor drugs. The present invention discloses a pyrimidine compound having a structure represented by a formula I, wherein W is NH, R1 is a nitrogen-containing five-membered heterocyclic ring, and R2 is a nitrogen-containing basic group. According to the present invention, the pyrimidine compound can inhibit a variety of tumor cells, can particularly and selectively act on EGFRL858R/T790M lung cancer cells, and can overcome the existing EGFR inhibitors, wherein the IC50 of the compounds is increased by 10-100 times compared to wild-type cells. The formula I is defined in the specification.