Month: October 2022

von Angerer, S. published the artcile< Product class 12: pyrimidines>, HPLC of Formula: 6554-61-6, 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. 6554-61-6 belongs to class pyrimidines, and the molecular formula is C4H2Cl2N2, HPLC of Formula: 6554-61-6.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Ma, Bin; Metrick, Claire M.; Gu, Chungang; Hoemberger, Marc; Bajrami, Bekim; Bame, Eris; Huang, Jiansheng; Mingueneau, Michael; Murugan, Paramasivam; Santoro, Joseph C.; Tang, Hao; Wang, Ti; Hopkins, Brian T. published the artcile< Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors>, HPLC of Formula: 5018-38-2, the main research area is piperazinone antiinflammatory BTK inhibitor autoimmune disease; B cell; BTK; Covalent inhibitor; Piperazinone; Selectivity; X-ray.

BTK is a tyrosine kinase playing an important role in B cell and myeloid cell functions through B cell receptor (BCR) signaling and Fc receptor (FcR) signaling. Selective inhibition of BTK has the potential to provide therapeutical benefits to patients suffering from autoimmune diseases. Here we report the design, optimization, and characterization of novel potent and highly selective covalent BTK inhibitors. Starting from a piperazinone hit derived from a selective reversible inhibitor, we solved the whole blood cellular potency issue by introducing an electrophilic warhead to reach Cys481. This design led to a covalent irreversible BTK inhibitor series with excellent kinase selectivity as well as good whole blood CD69 cellular potency. Optimization of metabolic stability led to representative compounds like 42, which demonstrated strong cellular target occupancy and inhibition of B-cell proliferation measured by proximal and distal functional activity.

Bioorganic & Medicinal Chemistry Letters published new progress about Autoimmune disease. 5018-38-2 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2O, HPLC of Formula: 5018-38-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Prusoff, William H.; Gaito, Raymond A. published the artcile< Effect of 6-azathymine, an analog of thymine, on the urinary excretion of uracil>, Recommanded Product: 6-Bromo-1,2,4-triazine-3,5(2H,4H)-dione, the main research area is NUCLEOSIDES AND NUCLEOTIDES/pharmacology; URACIL/urine.

Administration of 6-azathymine, an analog of thymine, to mice resulted in the excretion of large amounts of uracil in urine. 6-Azathymine and 5-bromo-6-azauracil, but not 6-azauracil, 5-ethyl-6-azauracil or 5-propyl-6azauracil inhibited the degradation of uracil by a particle-free fraction of rat liver. The enzyme degradation of uracil was inhibited by 6-azathymine to a greater extent than by thymine.

Biochimica et Biophysica Acta, Specialized Section on Nucleic Acids and Related Subjects published new progress about Enzymes Role: BIOL (Biological Study). 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Recommanded Product: 6-Bromo-1,2,4-triazine-3,5(2H,4H)-dione.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Mosrin, Marc; Knochel, Paul published the artcile< Regio- and Chemoselective Multiple Functionalization of Pyrimidine Derivatives by Selective Magnesiations using TMPMgCl·LiCl>, Product Details of C4H2Br2N2, the main research area is chlorotetramethylpiperidinylmagnesium lithium chloride magnesiation pyrimidine reaction electrophile.

Successive regio- and chemoselective magnesiations of pyrimidines using TMPMgCl·LiCl furnish, after trapping with various electrophiles, highly functionalized derivatives, e.g. I, in good to excellent yields. Applications to the synthesis of antiviral and anti-inflammatory agents such as p38 and sPLA2 kinase inhibitors are reported.

Organic Letters published new progress about Chemoselectivity. 3921-01-5 belongs to class pyrimidines, and the molecular formula is C4H2Br2N2, Product Details of C4H2Br2N2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Ibrahim, Hany S.; Abdelsalam, Mohamed; Zeyn, Yanira; Zessin, Matthes; Mustafa, Al-Hassan M.; Fischer, Marten A.; Zeyen, Patrik; Sun, Ping; Buelbuel, Emre F.; Vecchio, Anita; Erdmann, Frank; Schmidt, Matthias; Robaa, Dina; Barinka, Cyril; Romier, Christophe; Schutkowski, Mike; Kraemer, Oliver H.; Sippl, Wolfgang published the artcile< Synthesis, Molecular Docking and Biological Characterization of Pyrazine Linked 2-Aminobenzamides as New Class I Selective Histone Deacetylase (HDAC) Inhibitors with Anti-Leukemic Activity>, Electric Literature of 89793-12-4, the main research area is pyrazine linked aminobenzamide preparation SAR docking antileukemic HDAC inhibitor; 2-aminobenzamides; HDAC1; HDAC2; HDAC3; SAR studies; acute myeloid leukemia (AML); docking; histone deacetylases.

Synthesis of a novel series of class-I selective HDAC inhibitors (HDACi) containing a 2-aminobenzamide moiety as a zinc-binding group connected with a central (piperazin-1-yl)pyrazine or (piperazin-1-yl)pyrimidine moiety I [R1 = H, Me, CH2-2-pridinyl, etc.; R2 = H, F; R3 = H, F, Cl; X = CH, N; Y = CH, N], II [R4 = H, Me; R5 = H, F, 2-FC6H4, etc.; R6 = H, F, Cl, etc.] was reported. Some of the compounds were addnl. substituted with an aromatic capping group. Compounds I and II were tested in vitro against human HDAC1, 2, 3, and 8 enzymes and compared to reference class I HDACi (Entinostat (MS-275), Mocetinostat, CI994 and RGFP-966). The most promising compounds were found to be highly selective against HDAC1, 2 and 3 over the remaining HDAC subtypes from other classes. Mol. docking studies and MD simulations were performed to rationalize the in vitro data and to deduce a complete structure activity relationship (SAR) anal. of this novel series of class-I HDACi. The most potent compounds, including I [R1 = CH2-3-indolyl, etc.; R2 = H; R3 = H; X = CH; Y = N], which blocked HDAC1, HDAC2, and HDAC3, as well as the selective HDAC1/HDAC2 inhibitors II [R4 = H, (CH2)2-1-methyl-indol-3-yl; R5 = 2-thienyl; R6 = H] were selected for further cellular testing against human acute myeloid leukemia (AML) and erythroleukemic cancer (HEL) cells, took into consideration their low toxicity against human embryonic HEK293 cells. Compound I [R1 = CH2-3-indolyl, etc.; R2 = H; R3 = H; X = CH; Y = N] was superior to the clin. tested class-I HDACi Entinostat (MS-275). Thus, I [R1 = CH2-3-indolyl, etc.; R2 = H; R3 = H; X = CH; Y = N] was a new and specific HDACi with the potential to eliminate blood cancer cells of various origins.

International Journal of Molecular Sciences published new progress about Acids Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Electric Literature of 89793-12-4.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Li, Ruoxi; Ling, Dazheng; Tang, Tongke; Huang, Zhenghui; Wang, Manjiong; Mao, Fei; Zhu, Jin; Jiang, Lubin; Li, Jian; Li, Xiaokang published the artcile< Repurposing of antitumor drug candidate Quisinostat lead to novel spirocyclic antimalarial agents>, Safety of Ethyl 2-chloropyrimidine-5-carboxylate, the main research area is pyrimidine containing spirocyclic linker preparation cytotoxicity antimalarial human SAR.

Herein, 30 novel spirocyclic linker derivatives I [R = Ph, N-Me-indolin-2-yl, N-Me-6-F-indolin-3-yl, etc.] were designed and synthesized based on Quisinostat as lead compound and then evaluated for their antimalarial activities and cytotoxicity. Among them, compounds I [R = N-Me-indolin-2-yl, N-Me-6-F-indolin-3-yl] could effectively eliminate wild-type and multi-drug resistant P. falciparum parasites, and display weakened cytotoxicity and good metabolic stability. Western blot assay demonstrated that they could inhibit Plasmodium falciparum histone deacetylase (PfHDAC) activity like Quisinostat. In addition, both I [R = N-Me-indolin-2-yl, N-Me-6-F-indolin-3-yl] showed certain antimalarial efficacy in rodent malaria model, and the animal toxicity of I [R = N-Me-indolin-2-yl] was significantly improved compared with Quisinostat. Overall, I [R = N-Me-indolin-2-yl, N-Me-6-F-indolin-3-yl] were structurally novel PfHDAC inhibitors and provided prospective prototype for further antimalarial drug research.

Chinese Chemical Letters published new progress about Antimalarials. 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Safety of Ethyl 2-chloropyrimidine-5-carboxylate.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Al-Masoudi, Najim A.; Pfleiderer, Wolfgang; Lazrek, Hassan B. published the artcile< Synthesis of some novel 1-(5-thio-β-D-glucopyranosyl)-6-azauracil derivatives. Thio sugar nucleosides>, Quality Control of 4956-05-2, the main research area is thio sugar azauracil nucleoside; thioglucopyranosyl azauracil; glycosidation thioglucopyranose azauracil.

Title compounds I (R = H, Br, SBn, NHBn) were prepared via glycosidation of azauracil with thioglucopyranose derivatives

Nucleosides & Nucleotides published new progress about 4956-05-2. 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Quality Control of 4956-05-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Schweizer, Stefan A.; Bach, Thorsten published the artcile< Regioselective Pd(0)-catalyzed Hiyama cross-coupling reactions at dihalo-substituted heterocycles>, Product Details of C4H2Br2N2, the main research area is haloheterocycle regioselective Hiyama cross coupling alkyl fluorosilane palladium catalyst.

The regioselectivity of the Hiyama cross-coupling reaction at various dihalo-substituted heterocycles was studied. Me 2,3-dibromo-5-furancarboxylate and n-octyltrifluorosilane were employed to find optimum reaction conditions [CsF; Pd2dba3/P(2-furyl)3 as catalyst, 80-150 °C in toluene or benzene] for the desired transformation. Subsequent experiments with the title compounds and with different primary alkyltrifluorosilanes illustrate the generality of this regiochem. process.

Synlett published new progress about Haloalkyl silanes, fluoroalkyl Role: RCT (Reactant), RACT (Reactant or Reagent). 3921-01-5 belongs to class pyrimidines, and the molecular formula is C4H2Br2N2, Product Details of C4H2Br2N2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Wu, Xiao-qiong published the artcile< New method for synthesis of 4,6-dichloro-5-methoxypyrimidine>, Category: pyrimidines, the main research area is dichloro methoxypyrimidine aminolysis cyclization chlorination.

The research aimed to improve the synthesis method of 4,6-dichloro-5-methoxypyrimidine. 2-Methoxy di-Me malonate was used to prepare 4,6-dichloro-5- methoxypyrimidine by aminolysis, cyclization and chlorination. Results showed that the synthetic product was analyzed by IR spectrum, hydrogen NMR and mass spectrometry. The overall yield was 42%. It was concluded that the synthesis method was suitable for industrial production, because of its warm condition and higher yield.

Anhui Nongye Kexue published new progress about Aminolysis. 5018-38-2 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2O, Category: pyrimidines.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Miyakawa, Shin; Cleaves, H. James; Miller, Stanley L. published the artcile< The Cold Origin of Life: B. Implications Based on Pyrimidines and Purines Produced From Frozen Ammonium Cyanide Solutions>, Application In Synthesis of 15837-41-9, the main research area is ammonium cyanide purine pyrimidine life origin.

A wide variety of pyrimidines and purines were identified as products of a dilute frozen ammonium cyanide solution that had been held at -78° for 27 yr. This demonstrates that both pyrimidines and purines could have been produced on the primitive earth in a short time by eutectic concentration of HCN, even though the concentration of HCN in the primitive ocean may have been low. We suggest that eutectic freezing is the most plausible demonstrated mechanism by which HCN polymerizations could have produced biol. important prebiotic compounds

Origins of Life and Evolution of the Biosphere published new progress about Freezing (eutectic). 15837-41-9 belongs to class pyrimidines, and the molecular formula is C4H4N2O2, Application In Synthesis of 15837-41-9.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia