Category: 56-05-3

Meduna, Steven P. published the artcileTriamino pyrimidines and pyridines as histamine H₄ receptor modulators, Recommanded Product: 2-Amino-4,6-dichloropyrimidine, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(10), 3113-3116, database is CAplus and MEDLINE.

Two series of triamino pyrimidines and a series of triamino pyridines have been synthesized and their structure-activity relationships evaluated for activity at the H₄ receptor in competitive binding and functional assays. Small structural changes in these three hetereoarom. cores influenced the functional activity of these compounds

Bioorganic & 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, Recommanded Product: 2-Amino-4,6-dichloropyrimidine.

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

Zhao, Matthew M. published the artcileProcess Development of Tryptophan Hydroxylase Inhibitor LX1031, a Drug Candidate for the Treatment of Irritable Bowel Syndrome, Category: pyrimidines, the publication is Organic Process Research & Development (2020), 24(2), 261-273, database is CAplus.

Two process routes for LX1031 (I), a tryptophan hydroxylase inhibitor for the treatment of irritable bowel syndrome, were developed. They shared the same left-hand and right-hand starting materials as well as the penultimate intermediate. The chiral center in the left-hand moiety was established via a Noyori asym. hydrogenation of a trifluoromethyl aryl ketone. The right-hand boronate was prepared via a palladium-catalyzed borylation of L-tyrosine-derived aryl triflate. Union of these two fragments to the pyrimidine core, from the right- or left-hand side, constituted the first- and second-generation routes, resp. Removal of the Boc-protecting group from the penultimate intermediate gave LX1031. The challenges overcome in purification and isolation of the LX1031 zwitterion are also discussed. Both process routes were successfully performed on multikilogram scales to supply LX1031 API for the preclin. and clin. studies.

Organic Process Research & Development 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 C10H18O4, Category: pyrimidines.

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

Xuan, G. S. published the artcileInhibition of carbonic anhydrase II by sulfonamide derivatives, SDS of cas: 56-05-3, the publication is Pharmazie (2021), 76(9), 412-415, database is CAplus and MEDLINE.

A series of sulfonamide derivatives I [R = NH₂, ethoxycarbonylazanyl, (pyrimidin-2-yl)aminyl, 3-methyl-5-phenyl-1H-pyrazol-1-yl, etc.; R¹ = H, C(O)CH₃] were synthesized, and the enzyme inhibitory activity of the synthesized compounds I on carbonic anhydrase II was evaluated. Through mol. docking studies, it was found that compounds I [R = NHNH₂, R¹ = C(O)CH₃; R = (pyrimidin-2-yl)aminyl, R¹ = C(O)CH₃ (II); R = acetamidyl, R¹ = C(O)CH₃; R = ethoxycarbonylazanyl, R¹ = C(O)CH₃ (III); R = 3,5-dimethyl-1H-pyrazol-1-yl, R¹ = H (IV)] have a strong binding affinity to carbonic anhydrase II. The IC₅₀ values of the four compounds II, III, IV and I (R = 3-methyl-5-phenyl-1H-pyrazol-1-yl; R¹ = H) were lower than that of the pos. control drug acetazolamide. What’s more, the compounds had a high inhibitory activity for A549 lung cancer cell growth, among them, II and IV could inhibit both carbonic anhydrase II and lung cancer cell proliferation.

Pharmazie 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 C24H12, SDS of cas: 56-05-3.

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

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

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

Krasnov, Victor P. published the artcileSynthesis of Pyrimidine Conjugates with 4-(6-Amino-hexanoyl)-7,8-difluoro-3,4-dihydro-3-methyl-2H-[1,4]benzoxazine and Evaluation of Their Antiviral Activity, Application In Synthesis of 56-05-3, the publication is Molecules (2022), 27(13), 4236, database is CAplus and MEDLINE.

A series of pyrimidine conjugates containing a fragment of racemic 7,8-difluoro-3,4-dihydro-3-methyl-2H-[1,4]benzoxazine and its (S)-enantiomer attached via a 6-aminohexanoyl fragment were synthesized by the reaction of nucleophilic substitution of chlorine in various chloropyrimidines. Enantiomeric purity of optically active derivatives was confirmed by chiral HPLC. Antiviral evaluation of the synthesized compounds has shown that the replacement of purine with a pyrimidine fragment leads to a decrease in the anti-herpesvirus activity compared to the lead compound, purine conjugate. The studied compounds did not exhibit significant activity against influenza A (H1N1) virus.

Molecules 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

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

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

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