Tag: M.W=150-200

Zhang, Jing-Wen published the artcileDonor-acceptor carbon nitride with electron-withdrawing chlorine group to promote exciton dissociation, Name: 2-Amino-4,6-dichloropyrimidine, the publication is Chinese Journal of Catalysis (2021), 42(7), 1168-1175, database is CAplus.

Carbon nitride (C₃N₄) is promising for photocatalytic hydrogen production, but photogenerated electrons and holes in C₃N₄ usually tend to exist as excitons due to intrinsic Coulomb interactions making its photocatalytic activity unsatisfactory. Herein, a well-designed intramol. C₃N₄-based donor-acceptor (D-A) photocatalytic system was constructed to promote exciton dissociation Due to its good chem. compatibility with melamine and appropriate sublimation property, 2-amino-4,6-dichloropyrimidine unit was chosen as the monomer to react with melamine to construct intramol. D-A system (CNCl_x). The hydrogen evolution rate of CNCl_0.15 is 15.3 times higher than that of bulk C₃N₄ under visible light irradiation, with apparent quantum efficiency of 13.6% at 420 nm. The enhanced activity is attributed to introduced electron-withdrawing -Cl group as terminal group in the resulted CNCl_x samples, which can build internal elec. field to promote the exciton dissociation into free electron and hole. In addition, lower work function value of CNCl_x samples indicates that internal elec. field can help free electrons and holes transfer to the surface of CNCl_x samples for photocatalytic reaction.

Chinese Journal of Catalysis published new progress about 56-05-3. 56-05-3 belongs to pyrimidines, auxiliary class Pyrimidine,Chloride,Amine,API, name is 2-Amino-4,6-dichloropyrimidine, and the molecular formula is C15H14O3, Name: 2-Amino-4,6-dichloropyrimidine.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia

Burger, Matthew T. published the artcileIdentification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer, SDS of cas: 56-05-3, the publication is ACS Medicinal Chemistry Letters (2011), 2(10), 774-779, database is CAplus and MEDLINE.

Phosphoinositide-3-kinases (PI3Ks) are important oncol. targets due to the deregulation of this signaling pathway in a wide variety of human cancers. Herein we describe the structure guided optimization of a series of 2-morpholino, 4-substituted, 6-heterocyclic pyrimidines where the pharmacokinetic properties were improved by modulating the electronics of the 6-position heterocycle, and the overall druglike properties were fine-tuned further by modification of the 4-position substituent. The resulting 2,4-bismorpholino 6-heterocyclic pyrimidines are potent class I PI3K inhibitors showing mechanism modulation in PI3K dependent cell lines and in vivo efficacy in tumor xenograft models with PI3K pathway deregulation (A2780 ovarian and U87MG glioma). These efforts culminated in the discovery of 15 (NVP-BKM120), currently in Phase II clin. trials for the treatment of cancer.

ACS Medicinal Chemistry Letters published new progress about 56-05-3. 56-05-3 belongs to pyrimidines, auxiliary class Pyrimidine,Chloride,Amine,API, name is 2-Amino-4,6-dichloropyrimidine, and the molecular formula is C4H3Cl2N3, SDS of cas: 56-05-3.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia

Loksha, Yasser M. published the artcileSynthesis and Anti-HIV-1 Evaluation of Some Novel MC-1220 Analogs as Non-Nucleoside Reverse Transcriptase Inhibitors, Product Details of C6H9N3O2, the publication is Archiv der Pharmazie (Weinheim, Germany) (2016), 349(5), 363-372, database is CAplus and MEDLINE.

Some novel MC-1220 analogs were synthesized by a condensation of 4,6-dichloro-N-methylpyrimidin-2-amine derivatives and/or 4-chloro-6-methoxy-N,N,5-trimethylpyrimidin-2-amine with the sodium salt of 2,6-difluorophenylacetonitrile followed by treatment with aqueous sodium hydroxide in methanol, alkylation, reduction, halogenation, and/or acidic hydrolysis. All synthesized compounds were evaluated for their activity against HIV-1. The most active compound in this study showed activity against HIV-1 comparable to that of MC-1220. The only difference in structure between compound 7 and MC-1220 is a fluoro atom instead of a CH₃ group.

Archiv der Pharmazie (Weinheim, Germany) published new progress about 5738-14-7. 5738-14-7 belongs to pyrimidines, auxiliary class Pyrimidine,Amine,Alcohol,Pyrimidine, name is 2-(Dimethylamino)pyrimidine-4,6-diol, and the molecular formula is C6H9N3O2, Product Details of C6H9N3O2.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia

Li, Wei published the artcileSynthesis and biological activity evaluation of imidazole heterocyclic sulfonylurea compounds, Related Products of pyrimidines, the publication is Heterocycles (2021), 102(7), 1374-1384, database is CAplus.

Sulfonylurea herbicides are the most widely used herbicides in the world. They have the advantages of high efficiency, good selectivity, and no toxicity to human and animals. In this study, sulfonylureas containing imidazole heterocycles were synthesized on the basis of computer simulation of mol. docking, and the biol. activity was evaluated. It shows that the compound has a good inhibitory effect on the ALS and a certain inhibitory effect on the phytopathogenic fungi of Curvularia lunata and Curvularia mebaldsii. Its inhibitory rate at concentration of 50 mg/L is similar to that of the carbendazim. This research provides the basis for further optimization of the structure of imidazolium heterocyclic sulfonylurea and the synthesis of its derivatives

Heterocycles published new progress about 56-05-3. 56-05-3 belongs to pyrimidines, auxiliary class Pyrimidine,Chloride,Amine,API, name is 2-Amino-4,6-dichloropyrimidine, and the molecular formula is C4H3Cl2N3, Related Products of pyrimidines.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia

Hill, Zachary B. published the artcileTargeting Diverse Signaling Interaction Sites Allows the Rapid Generation of Bivalent Kinase Inhibitors, Application In Synthesis of 56-05-3, the publication is ACS Chemical Biology (2012), 7(3), 487-495, database is CAplus and MEDLINE.

The identification of potent and selective modulators of protein kinase function remains a challenge, and new strategies are needed for generating these useful ligands. Here, we describe the generation of bivalent inhibitors of three unrelated protein kinases: the CAMK family kinase Pim1, the mitogen-activated protein kinase (MAPK) p38α, and the receptor tyrosine kinase (RTK) epidermal growth factor receptor (EGFR). These bivalent inhibitors consist of an ATP-competitive inhibitor that is covalently tethered to an engineered form of the self-labeling protein O⁶-alkylguanine-DNA alkyltransferase (SNAP-tag). In each example, SNAP-tag is fused to a peptide ligand that binds to a signaling interaction site of the kinase being targeted. These interactions increase the overall selectivity and potency of the bivalent inhibitors that were generated. The ability to exploit disparate binding sites in diverse kinases points to the generality of the method described. Finally, we demonstrate that ATP-competitive inhibitors that are conjugated to the bio-orthogonal tag O⁴-benzyl-2-chloro-6-aminopyrimidine (CLP) are cell-permeable. The selective labeling of SNAP-tag with CLP conjugates allows the rapid assembly of bivalent inhibitors in living cells.

ACS Chemical Biology published new progress about 56-05-3. 56-05-3 belongs to pyrimidines, auxiliary class Pyrimidine,Chloride,Amine,API, name is 2-Amino-4,6-dichloropyrimidine, and the molecular formula is C4H3Cl2N3, Application In Synthesis of 56-05-3.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia

Tardibono, Lawrence P. Jr. published the artcileEnantioselective syntheses of carbocyclic nucleosides 5′-homocarbovir, epi-4′-homocarbovir, and their cyclopropylamine analogs using facially selective Pd-mediated allylations, Recommanded Product: 2-Amino-4,6-dichloropyrimidine, the publication is Tetrahedron (2011), 67(5), 825-829, database is CAplus and MEDLINE.

Carbocyclic nucleosides (-)-5′-homocarbovir and (+)-epi-4′-homocarbovir were prepared from an acylnitroso-derived hetero Diels-Alder cycloadduct. A kinetic enzymic resolution generated an enantiopure aminocyclopentenol and Pd(0)-mediated decarboxylative allylations of allyl 2,2,2-trifluoroethyl malonates were used to install the 4′-hydroxyethyl groups. Late stage derivatization gave access to the cyclopropylamine analogs, (-)-5′-homoabacavir, and (+)-epi-4′-homoabacavir. All carbonucleoside target mols. were evaluated for antiviral activity.

Tetrahedron published new progress about 56-05-3. 56-05-3 belongs to pyrimidines, auxiliary class Pyrimidine,Chloride,Amine,API, name is 2-Amino-4,6-dichloropyrimidine, and the molecular formula is C3H7NO2, Recommanded Product: 2-Amino-4,6-dichloropyrimidine.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia

Grant, Jennifer published the artcileAn Immobilized Enzyme Reactor for Spatiotemporal Control over Reaction Products, Product Details of C4H3Cl2N3, the publication is Small (2018), 14(31), n/a, database is CAplus and MEDLINE.

This paper describes a microfluidic chip wherein the position and order of two immobilized enzymes affects the type and quantity of reaction products in the flowing fluid. Assembly of the chip is based on a self-assembled monolayer presenting two orthogonal covalent capture ligands that immobilize their resp. fusion enzyme. A thiol-tagged substrate is flowed over a region presenting the first enzyme – which generates a product that is efficiently transferred to the second enzyme – and the second enzyme’s product binds to an adjacent thiol capture site on the chip. The amount of the three possible reaction products is quantified directly on the chip using self-assembled monolayers for matrix-assisted laser desorption/ionization mass spectrometry, revealing that the same microsystem can be spatiotemporally arranged to produce different products depending on the device design. This work allows for optimizing multistep biochem. transformations in favor of a desired product using a facile reaction and anal. format.

Small published new progress about 56-05-3. 56-05-3 belongs to pyrimidines, auxiliary class Pyrimidine,Chloride,Amine,API, name is 2-Amino-4,6-dichloropyrimidine, and the molecular formula is C4H3Cl2N3, Product Details of C4H3Cl2N3.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia

Lee, Jinho published the artcile3,5-Bis(aminopyrimidinyl)indole Derivatives: Synthesis and Evaluation of Pim Kinase Inhibitory Activities, Quality Control of 56-05-3, the publication is Bulletin of the Korean Chemical Society (2014), 35(7), 2123-2129, database is CAplus.

A novel series of 3,5-bis(aminopyrimidinyl)indole derivatives I (R = (CH₃)₂N(CH₂)₂O, cyclopentyloxy, Me piperazinyl, etc.) were synthesized and evaluated against Pim kinases, meridianin C was chosen as a hit structure and its substituent was modified to discover potent and selective pan-pim kinase inhibitors. Substitution at C-5-position by 2-amino-pyrimidine having hydrophilic aminoalkyl chain improved the potency were described. SAR o f substituents at C-4 position of 2-amino-pyrimidine suggested that aminoalkyl moiety, with the adequate chain length and substituent, could provide compound with the high potency and selectivity. This study suggests the 3,5-bis(aminopyrimidinyl)indole moiety is a very interesting scaffold, which can be further optimized for more potent inhibitors of pim kinases.

Bulletin of the Korean Chemical Society published new progress about 56-05-3. 56-05-3 belongs to pyrimidines, auxiliary class Pyrimidine,Chloride,Amine,API, name is 2-Amino-4,6-dichloropyrimidine, and the molecular formula is C4H3Cl2N3, Quality Control of 56-05-3.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia

Tardibono, Lawrence P. Jr. published the artcileEnantioselective syntheses of carbocyclic nucleosides 5′-homocarbovir, epi-4′-homocarbovir, and their cyclopropylamine analogs using facially selective Pd-mediated allylations, Recommanded Product: 2-Amino-4,6-dichloropyrimidine, the publication is Tetrahedron (2011), 67(5), 825-829, database is CAplus and MEDLINE.

Carbocyclic nucleosides (-)-5′-homocarbovir and (+)-epi-4′-homocarbovir were prepared from an acylnitroso-derived hetero Diels-Alder cycloadduct. A kinetic enzymic resolution generated an enantiopure aminocyclopentenol and Pd(0)-mediated decarboxylative allylations of allyl 2,2,2-trifluoroethyl malonates were used to install the 4′-hydroxyethyl groups. Late stage derivatization gave access to the cyclopropylamine analogs, (-)-5′-homoabacavir, and (+)-epi-4′-homoabacavir. All carbonucleoside target mols. were evaluated for antiviral activity.

Tetrahedron published new progress about 56-05-3. 56-05-3 belongs to pyrimidines, auxiliary class Pyrimidine,Chloride,Amine,API, name is 2-Amino-4,6-dichloropyrimidine, and the molecular formula is C3H7NO2, Recommanded Product: 2-Amino-4,6-dichloropyrimidine.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia

Grant, Jennifer published the artcileAn Immobilized Enzyme Reactor for Spatiotemporal Control over Reaction Products, Product Details of C4H3Cl2N3, the publication is Small (2018), 14(31), n/a, database is CAplus and MEDLINE.

This paper describes a microfluidic chip wherein the position and order of two immobilized enzymes affects the type and quantity of reaction products in the flowing fluid. Assembly of the chip is based on a self-assembled monolayer presenting two orthogonal covalent capture ligands that immobilize their resp. fusion enzyme. A thiol-tagged substrate is flowed over a region presenting the first enzyme – which generates a product that is efficiently transferred to the second enzyme – and the second enzyme’s product binds to an adjacent thiol capture site on the chip. The amount of the three possible reaction products is quantified directly on the chip using self-assembled monolayers for matrix-assisted laser desorption/ionization mass spectrometry, revealing that the same microsystem can be spatiotemporally arranged to produce different products depending on the device design. This work allows for optimizing multistep biochem. transformations in favor of a desired product using a facile reaction and anal. format.

Small published new progress about 56-05-3. 56-05-3 belongs to pyrimidines, auxiliary class Pyrimidine,Chloride,Amine,API, name is 2-Amino-4,6-dichloropyrimidine, and the molecular formula is C4H3Cl2N3, Product Details of C4H3Cl2N3.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia