Category: 99469-85-9

Farina, Vittorio; Krishnamurthy, Venkat; Scott, William J. published the artcile< The Stille reaction>, COA of Formula: C5H4Cl2N2S, the main research area is review Reaction; review Stille.

A review of the article The Stille reaction.

Organic Reactions (Hoboken, NJ, United States) published new progress about Organic synthesis. 99469-85-9 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2S, COA of Formula: C5H4Cl2N2S.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Solberg, Jan; Undheim, Kjell published the artcile< Regiochemistry in palladium-catalyzed organotin reactions with halopyrimidines>, Recommanded Product: 4,5-Dichloro-2-(methylthio)pyrimidine, the main research area is halopyrimidine coupling organotin palladium catalyzed; regiochem halopyrimidine coupling organotin.

Chlorines in activated pyrimidine position are replaced by carbon substituents in Pd-catalyzed reactions with organotin compounds The 4(6)-position is more reactive than the 2-position allowing for regioselective coupling in 2,4(6)-dihalopyrimidines. A bromine substituent is required for coupling in the benzenoid 5-position. In 5-bromo-2,4-dichloropyrimidine the 4-chlorine is replaced before the 5-bromine and the latter before the 2-chlorine substituent, all in a regioselective manner. The methodol. can be used to introduce functionalized carbon substituents into any pyrimidine position.

Acta Chemica Scandinavica published new progress about Coupling reaction. 99469-85-9 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2S, Recommanded Product: 4,5-Dichloro-2-(methylthio)pyrimidine.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Lebraud, Honorine; Wright, David J.; East, Charlotte E.; Holding, Finn P.; O’Reilly, Marc; Heightman, Tom D. published the artcile< In-gel activity-based protein profiling of a clickable covalent ERK1/2 inhibitor>, Name: 4,5-Dichloro-2-(methylthio)pyrimidine, the main research area is in gel activity based protein profiling ERK1 ERK2.

In-gel activity-based protein profiling (ABPP) offers rapid assessment of the proteome-wide selectivity and target engagement of a chem. tool. Here we demonstrate the use of the inverse electron demand Diels Alder (IEDDA) click reaction for in-gel ABPP by evaluating the selectivity profile and target engagement of a covalent ERK1/2 probe tagged with a trans-cyclooctene group. The chem. probe was shown to bind covalently to Cys166 of ERK2 using protein MS and X-ray crystallog., and displayed submicromolar GI50s in A375 and HCT116 cells. In both cell lines, the probe demonstrated target engagement and a good selectivity profile at low concentrations, which was lost at higher concentrations The IEDDA cycloaddition enabled fast and quant. fluorescent tagging for readout with a high background-to-noise ratio and thereby provides a promising alternative to the commonly used copper catalyzed alkyne-azide cycloaddition

Molecular BioSystems published new progress about Click chemistry. 99469-85-9 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2S, Name: 4,5-Dichloro-2-(methylthio)pyrimidine.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Solberg, Jan; Undheim, Kjell published the artcile< Palladium catalysis in the preparation of alkynylpyrimidines>, Related Products of 99469-85-9, the main research area is iodopyrimidine alkyne coupling; palladium complex catalyst coupling; alkynylpyrimidine; pyrimidine alkynyl.

Coupling reaction of iodopyrimidines I (R = SMe, OSiMe3; R1 = iodo) with R2CCH (e.g., R2 = Ph, Bu) using Pd catalysts gave alkynylpyrimidines I (R1 = CCR2). Hydrolysis of I (R = OSiMe3, R1 = CCR2) with H2O at room temperature gave pyrimidinones II. m-ClC6H4C(O)OOH oxidn of I (R = SMe, R1 = CCR2) gave I (R = SO2Me). I (R = SO2Me, R1 = CCPh) on alk. hydrolysis gave II (R2 = Ph).

Acta Chemica Scandinavica, Series B: Organic Chemistry and Biochemistry published new progress about Coupling reaction. 99469-85-9 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2S, Related Products of 99469-85-9.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Bellenie, Benjamin R.; Cheung, Kwai-Ming J.; Varela, Ana; Pierrat, Olivier A.; Collie, Gavin W.; Box, Gary M.; Bright, Michael D.; Gowan, Sharon; Hayes, Angela; Rodrigues, Matthew J.; Shetty, Kartika N.; Carter, Michael; Davis, Owen A.; Henley, Alan T.; Innocenti, Paolo; Johnson, Louise D.; Liu, Manjuan; de Klerk, Selby; Le Bihan, Yann-Vai; Lloyd, Matthew G.; McAndrew, P. Craig; Shehu, Erald; Talbot, Rachel; Woodward, Hannah L.; Burke, Rosemary; Kirkin, Vladimir; van Montfort, Rob L. M.; Raynaud, Florence I.; Rossanese, Olivia W.; Hoelder, Swen published the artcile< Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders>, Formula: C5H4Cl2N2S, the main research area is preparation benzimidazolone inhibitor BCL6 interaction repressor lymphoma.

Deregulation of the transcriptional repressor BCL6 enables tumorigenesis of germinal center B-cells, and hence BCL6 has been proposed as a therapeutic target for the treatment of diffuse large B-cell lymphoma (DLBCL). Herein we report the discovery of a series of benzimidazolone inhibitors of the protein-protein interaction between BCL6 and its co-repressors. A subset of these inhibitors were found to cause rapid degradation of BCL6, and optimization of pharmacokinetic properties led to the discovery of 5-((5-chloro-2-((3R,5S)-4,4-difluoro-3,5-dimethylpiperidin-1-yl)pyrimidin-4-yl)amino)-3-(3-hydroxy-3-methylbutyl)-1-methyl-1,3-dihydro-2H-benzo[d]imidazol-2-one (CCT369260), which reduces BCL6 levels in a lymphoma xenograft mouse model following oral dosing.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 99469-85-9 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2S, Formula: C5H4Cl2N2S.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

von Angerer, S. published the artcile< Product class 12: pyrimidines>, Synthetic Route of 99469-85-9, the main research area is review pyrimidine preparation cyclization ring transformation aromatization.

A review. Methods for preparing pyrimidines are reviewed including cyclization, ring transformation, aromatization and substituent modification.

Science of Synthesis published new progress about Aromatization. 99469-85-9 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2S, Synthetic Route of 99469-85-9.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Adding a certain compound to certain chemical reactions, such as: 99469-85-9, 4,5-Dichloro-2-(methylthio)pyrimidine, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound, Safety of 4,5-Dichloro-2-(methylthio)pyrimidine, blongs to pyrimidines compound. Safety of 4,5-Dichloro-2-(methylthio)pyrimidine

Compound 51. To a mixture of compound 49 (976 mg, 5.13 mmol, 2 eq.), compound 50 (0.5 g, 2.56 mmol, 1 eq.) , Pd(PPh3)2Cl2 (360 mg, 512 mumol, 0.2 eq.), and CuI (244 mg, 1.28 mmol, 0.5 eq.) in THF (10 mL) was added TBAF (1 M, 2.56 mL, 1 eq.) in one portion at 0 C under N2. The reaction mixture was stirred at 60 C under N2 for 10 h. The mixture was partitioned between H2O(100 mL) and EtOAc(200 mL). The combined organic phase were washed with brine (200 mL), dried over Na2SO4, and concentrated in vacuo. The residue was purified by column chromatography (SiO2, PE/EtOAc: 1/0 to 50 /1) and prep- TLC (PE/EtOAc: 20:1) to afford compound 51 (0.3 g, 1.26 mmol, 49% yield) as a brown oil. 1H NMR (CDCl3, 400 MHz) delta 8.47 (s, 1H), 2.61 (d, J = 5.9 Hz, 2H), 2.56 (s, 3H), 1.13-1.03 (m, 1H), 0.61-0.52 (m, 2H), 0.36 (q, J = 4.9 Hz, 2H).

The synthetic route of 99469-85-9 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD.; SNIR-ALKALAY, Irit; VACCA, Joseph; BEN-NERIAH, Yinon; (238 pag.)WO2019/155468; (2019); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia