155-90-8Relevant academic research and scientific papers
Highly efficient, chemoselective syntheses of 2-methoxy-4-substituted pyrimidines
Xu, Chunyan,Cheng, Chuanjie,Liu, Hongtao,Liu, Bo
, p. 545 - 548 (2011)
Three 2-methoxy-4-substituted pyrimidine compounds were chemoselectively synthesized by diazotization, using 2,4-dichloropyrimidine as the starting material. In nonaqueous diazotization reaction system, halo-substituted 6 and 7 were efficiently prepared, and in aqueous medium, hydrolysis product 8 was afforded.
Synthesis and biological evaluation of novel flexible nucleoside analogues that inhibit flavivirus replication in vitro
Thames, Joy E.,Waters, Charles D.,Valle, Coralie,Bassetto, Marcella,Aouadi, Wahiba,Martin, Baptiste,Selisko, Barbara,Falat, Arissa,Coutard, Bruno,Brancale, Andrea,Canard, Bruno,Decroly, Etienne,Seley-Radtke, Katherine L.
, (2020)
Flaviviruses, such as Dengue (DENV) and Zika (ZIKV) viruses, represent a severe health burden. There are currently no FDA-approved treatments, and vaccines against most flaviviruses are still lacking. We have developed several flexible analogues (“fleximers”) of the FDA-approved nucleoside Acyclovir that exhibit activity against various RNA viruses, demonstrating their broad-spectrum potential. The current study reports activity against DENV and Yellow Fever Virus (YFV), particularly for compound 1. Studies to elucidate the mechanism of action suggest the flex-analogue triphosphates, especially 1-TP, inhibit DENV and ZIKV methyltransferases, and a secondary, albeit weak, effect on the DENV RNA-dependent RNA polymerase was observed at high concentrations. The results of these studies are reported herein.
Phototransformation of Chlorimuron-ethyl in Aqueous Solution
Choudhury, Partha P.,Dureja, Prem
, p. 3379 - 3382 (1996)
Chlorimuron-ethyl is relatively stable in water buffered to pH 7.0 and 9.0, but hydrolyzes readily (half-life, 14 d) in water buffered to pH 4.0. In addition, chlorimuron-ethyl photodegrades rapidly and extensively in aqueous solution. The predominant photoproducts are 4-methoxy-6-chloro-2-aminopyrimidine, ethyl 2-aminosulfonylbenzoate, N-(4-methoxy-6-chloropyrimidin-2-yl)methyl urea, and o-benzoic sulfimide (saccharin). A minor deesterified product (chlorimuron) was evident. The decrease in chlorimuron-ethyl concentration in aqueous solutions followed first-order kinetics. The rate of degradation in different types of water followed the order irrigation water > tap water > distilled water. Chlorimuron-ethyl photodegraded in pH 4, 7, and 9 buffer solutions under both UV and sunlight. A faster degradation rate in pH 4.0 buffer solution was observed.
C2-Selective, Functional-Group-Divergent Amination of Pyrimidines by Enthalpy-Controlled Nucleophilic Functionalization
Ham, Won Seok,Choi, Hoonchul,Zhang, Jianbo,Kim, Dongwook,Chang, Sukbok
supporting information, p. 2885 - 2892 (2022/02/23)
Synthesis of heteroaryl amines has been an important topic in organic chemistry because of their importance in small-molecule discovery. In particular, 2-Aminopyrimidines represent a highly privileged structural motif that is prevalent in bioactive molecules, but a general strategy to introduce the pyrimidine C2-N bonds via direct functionalization is elusive. Here we describe a synthetic platform for site-selective C-H functionalization that affords pyrimidinyl iminium salt intermediates, which then can be transformed into various amine products in situ. Mechanism-based reagent design allowed for the C2-selective amination of pyrimidines, opening the new scope of site-selective heteroaryl C-H functionalization. Our method is compatible with a broad range of pyrimidines with sensitive functional groups and can access complex aminopyrimidines with high selectivity.
2-MORPHOLIN-4,6-DISUBSTITUTED PYRIMIDINE DERIVATIVE, AND PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
-
Paragraph 0108, (2017/11/11)
Disclosed is a 2-morpholin-4,6-disubstituted pyrimidine derivative as shown in formula (I) below, and a pharmaceutically acceptable salt, solvate, stereoisomer or prodrug thereof, and a pharmaceutical composition thereof and a use thereof, wherein the definition of each group is as shown in the description. The compound has a PI3K kinase inhibition activity, and has a relatively high inhibitive ability and a low cytotoxicity against PIK3CA mutant breast cancer cell strains T47D and MCF-7.
DIBENZOOXEPIN DERIVATIVE
-
Paragraph 0372, (2014/06/24)
A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like,
Peptide deformylase inhibitors
-
Page/Page column, (2014/12/09)
The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
PEPTIDE DEFORMYLASE INHIBITORS
-
Page/Page column, (2014/02/15)
The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhi-bition of bacterial peptide deformylase (PDF) activity
Synthesis and evaluation of novel monosubstituted sulfonylurea derivatives as antituberculosis agents
Pan, Li,Jiang, Ying,Liu, Zhen,Liu, Xing-Hai,Liu, Zhuo,Wang, Gang,Li, Zheng-Ming,Wang, Di
experimental part, p. 18 - 26 (2012/07/01)
A series of novel monosubstituted sulfonylurea derivatives 10a-y were synthesized and characterized by 1H NMR, 13C NMR and HRMS. These compounds were evaluated against Mycobacterium tuberculosis H37Rv in vitro. The results showed compounds 10f, 10k and 10s exhibited moderate antituberculosis activities with MIC values in the range of 20-100 mg/L. Compounds 10b and 10o displayed good antituberculosis activities (MIC 10 mg/L), which were comparable with that of the sulfometuron methyl. Both of the two compounds showed little cytotoxicities, with an IC50 against THP-1 cells greater than 100 mg/L.
SUBSTITUTED IMIDAZO[1,2-A]PYRIMIDINES AND -PYRIDINES
-
Page/Page column 90; 91, (2012/02/02)
Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
