7470-50-0Relevant academic research and scientific papers
Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity
Teng, Yu,Li, Xinyu,Ren, Shengnan,Cheng, Yu,Xi, Kun,Shen, Hongtao,Ma, Wenzhuo,Luo, Guoshun,Xiang, Hua
, (2020/10/02)
Inhibition of PI3Kδ has been proved to be an efficacious strategy for the treatment of hematological malignancies where the PI3K/Akt signaling pathway is hyperactive. Herein, a series of quinazoline derivatives bearing acrylamide fragment were prepared using skeleton-deconstruction strategy. The preliminary bioactivity evaluation resulted in the discovery of lead compound 15c. Compound 15c exhibited excellent enzyme activity against PI3Kδ (IC50 = 27.5 nM) compared with BEZ235 as well as the significant anti-proliferation activities. With the high selectivity over other PI3K isoforms and potent effects on PI3K/Akt pathway, 15c can be identified as a promising PI3Kδ inhibitor worthy of further profiling.
Heteroaromatic compound and application thereof to drug
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Paragraph 0453; 0602; 0603; 0604; 0605, (2017/07/31)
The invention discloses a heteroaromatic compound and application thereof to drug. In particular, the invention provides a heteroaromatic compound or stereoisomers thereof, geometric isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, and a pharmaceutical composition comprising the compound provided by the invention. The invention also discloses application of the compound provided by the invention or the pharmaceutical composition thereofto preparation of a medicine for reatment of autoimmune diseases or proliferative diseases.
An efficient protocol for the amidation of carboxylic acids promoted by trimethyl phosphite and iodine
Luo, Qun-Li,Lv, Lina,Li, Yu,Tan, Jian-Ping,Nan, Wenhui,Hui, Qun
supporting information; experimental part, p. 6916 - 6922 (2012/01/06)
A practical, one-pot protocol is described for the conversion of carboxylic acids into amides through carboxyl activation by the reagent combination of trimethyl phosphite and iodine. This method integrates several advantages: (1) it allows amines to be chemoselectively acylated with excellent results in the presence of sulfur and oxygen nucleophiles; (2) the method shows wide generality in respect of solvent, base, and substrate; (3) the reagents used are widely available and much less expensive than common coupling reagents, and (4) the process is remarkably convenient, permitting extraction, recrystallization, and column chromatography as optional work-up procedures. The chemoselectivity and generality of the method, the low cost, and wide availability of reagents combined with the ease of use make it a very favorable process.
Synthesis and NMR-spectral characterization of N,N-dialkyl-3-nitroanilines, N,N-dialkyl-1,3-benzenediamines and their acyl derivatives
Katritzky, Alan R.,Rachwal, Bogumila,Rachwal, Stanislaw
, p. 337 - 345 (2007/10/02)
A recently discovered method for the synthesis of N,N-dialkyl-1,3-benzenediamines with two different alkyl groups is shown to be general.This is demonstrated by the synthesis of N-butyl-N-phenethyl-1,3-benzenediamine by the condensation of 3-nitroaniline with phenylacetaldehyde and benzotriazole, reduction of the adduct with sodium borohydride, acylation of the resulting N-phenethyl-3-nitroaniline with butyryl chloride, catalytic reduction of the nitro group by formic acid in the presence of triethylamine and palladium and finally reduction of the butyramide carbonyl group to the butyl substituent by lithium aluminium hydride.Several other routes were less efficient or failed completely.Classical methods for the synthesis of N,N-diethyl-1,3-benzenediamine were reexamined and improved.The recommended procedure involves alkylation of 3-nitroaniline with diethyl sulfate, trapping of N-ethyl-3-nitroaniline (by-product) by benzoylation, distillation of N,N-diethyl-3-nitro-aniline under reduced pressure and reduction of the nitro group by formic acid catalyzed by palladium.
