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Avitabile, Concetta’s team published research in Bioconjugate Chemistry in 26 | CAS: 186046-81-1

Bioconjugate Chemistry published new progress about 186046-81-1. 186046-81-1 belongs to pyrimidines, auxiliary class Pyrimidine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(4-(((benzhydryloxy)carbonyl)amino)-2-oxopyrimidin-1(2H)-yl)acetamido)acetic acid, and the molecular formula is C39H35N5O8, Recommanded Product: 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(4-(((benzhydryloxy)carbonyl)amino)-2-oxopyrimidin-1(2H)-yl)acetamido)acetic acid.

Avitabile, Concetta published the artcileIncorporation of Naked Peptide Nucleic Acids into Liposomes Leads to Fast and Efficient Delivery, Recommanded Product: 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(4-(((benzhydryloxy)carbonyl)amino)-2-oxopyrimidin-1(2H)-yl)acetamido)acetic acid, the publication is Bioconjugate Chemistry (2015), 26(8), 1533-1541, database is CAplus and MEDLINE.

The delivery of peptide nucleic acids (PNAs) to cells is a very challenging task. We report here that a liposomal formulation composed of egg PC/cholesterol/DSPE-PEG2000 can be loaded, according to different encapsulation techniques, with PNA or fluorescent PNA oligomers. PNA loaded liposomes efficiently and quickly promote the uptake of a PNA targeting the microRNA miR-210 in human erythroleukemic K562 cells. By using this innovative delivery system for PNA, down-regulation of miR-210 is achieved at a low PNA concentration

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

Avitabile, Concetta’s team published research in Bioconjugate Chemistry in 26 | CAS: 169396-92-3

Bioconjugate Chemistry published new progress about 169396-92-3. 169396-92-3 belongs to pyrimidines, auxiliary class Pyrimidine,Carboxylic acid,Amine,Amide,Others,PNA, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamido)acetic acid, and the molecular formula is C26H26N4O7, Formula: C26H26N4O7.

Avitabile, Concetta published the artcileIncorporation of Naked Peptide Nucleic Acids into Liposomes Leads to Fast and Efficient Delivery, Formula: C26H26N4O7, the publication is Bioconjugate Chemistry (2015), 26(8), 1533-1541, database is CAplus and MEDLINE.

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

Maimaitiyiming, Xieraili’s team published research in Materials Chemistry and Physics in 240 | CAS: 56-05-3

Materials Chemistry and Physics 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, Safety of 2-Amino-4,6-dichloropyrimidine.

Maimaitiyiming, Xieraili published the artcileSynthesis, characterization and properties of poly(2,5-didodecyloxy-1,4-diethynyl-phenylene-alt-2-N,N-dimethyl amino-4,6-pyrimidine), Safety of 2-Amino-4,6-dichloropyrimidine, the publication is Materials Chemistry and Physics (2020), 122116, database is CAplus.

This study reports the synthesis and characterization of new type π-conjugated poly(2,5-didodecyloxy-1,4- diethynyl-phenylene-alt-2-N,N-dimethyl amino-4,6-pyrimidine) with good acidochromism. This polymer was prepared by polycondensation of Sonogashira. Sonogashira was a general route for the preparation of arylacetylenes by coupling an alkynes with aryl or alkenyl halide (or triflates). There were very well solubility for the derivatized copolymer in general organic solvents and exhibits good thermal stability. The copolymer emits blue light under UV irradiation of the solution phase and when protonated with an organic acid, the copolymer exhibits a red shift. In addition, was detected that the copolymers with good acidochromism with acidic place. It was expected to used for acid recognition.

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

Hodges, Timothy R.’s team published research in Journal of Medicinal Chemistry in 61 | CAS: 1370001-96-9

Journal of Medicinal Chemistry published new progress about 1370001-96-9. 1370001-96-9 belongs to pyrimidines, auxiliary class Boronic acid and ester,Boronic acid and ester, name is 4-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidine, and the molecular formula is C11H17BN2O2, Formula: C11H17BN2O2.

Hodges, Timothy R. published the artcileDiscovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS, Formula: C11H17BN2O2, the publication is Journal of Medicinal Chemistry (2018), 61(19), 8875-8894, database is CAplus and MEDLINE.

Son of sevenless homolog 1 (SOS1) is a guanine nucleotide exchange factor that catalyzes the exchange of GDP for GTP on RAS. In its active form, GTP-bound RAS is responsible for numerous critical cellular processes. Aberrant RAS activity is involved in ∼30% of all human cancers; hence, SOS1 is an attractive therapeutic target for its role in modulating RAS activation. Here, we describe a new series of benzimidazole-derived SOS1 agonists. Using structure-guided design, we discovered small mols. that increase nucleotide exchange on RAS in vitro at submicromolar concentrations, bind to SOS1 with low double-digit nanomolar affinity, rapidly enhance cellular RAS-GTP levels, and invoke biphasic signaling changes in phosphorylation of ERK 1/2. These compounds represent the most potent series of SOS1 agonists reported to date.

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

Degorce, Sebastien L.’s team published research in Bioorganic & Medicinal Chemistry in 28 | CAS: 1370001-96-9

Bioorganic & Medicinal Chemistry published new progress about 1370001-96-9. 1370001-96-9 belongs to pyrimidines, auxiliary class Boronic acid and ester,Boronic acid and ester, name is 4-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidine, and the molecular formula is C11H17BN2O2, Related Products of pyrimidines.

Degorce, Sebastien L. published the artcileImproving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors, Related Products of pyrimidines, the publication is Bioorganic & Medicinal Chemistry (2020), 28(23), 115815, database is CAplus and MEDLINE.

In this article, we report our efforts towards improving in vitro human clearance in a series of 5-azaquinazolines through a series of C4 truncations and C2 expansions. Extensive DMPK studies enabled us to tackle high Aldehyde Oxidase (AO) metabolism and unexpected discrepancies in human hepatocyte and liver microsomal intrinsic clearance. Our efforts culminated with the discovery of 5-azaquinazoline I, which also displayed exquisite selectivity for IRAK4, and showed synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with the covalent BTK inhibitor acalabrutinib.

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

Roth, Barbara’s team published research in Journal of Medicinal Chemistry in 1980-05-31 | CAS: 73576-33-7

Journal of Medicinal Chemistry published new progress about pyrimidinediamine benzyl preparation bactericide; bactericide benzylpyrimidinediamine; dihydrofolate reductase benzylpyrimidinediamine; trimethoprim derivative benzylpyrimidinediamine. 73576-33-7 belongs to class pyrimidines, name is 4-Chloro-6-isopropylpyrimidin-2-amine, and the molecular formula is C7H10ClN3, Product Details of C7H10ClN3.

Roth, Barbara published the artcile2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 4. 6-Substituted trimethoprim derivatives from phenolic Mannich intermediates. Application to the synthesis of trimethoprim and 3,5-dialkylbenzyl analogs, Product Details of C7H10ClN3, the main research area is pyrimidinediamine benzyl preparation bactericide; bactericide benzylpyrimidinediamine; dihydrofolate reductase benzylpyrimidinediamine; trimethoprim derivative benzylpyrimidinediamine.

The preparation of a wide variety of 6-substituted trimethoprim analogs was readily accomplished by the reaction of 6-substituted 2,4-diaminopyrimidines with 2,6-dimethoxy-4-[(dimethylamino)methyl]phenol at 120-160°. The less reactive 2,6-dialkyl-4-[(dimethylamino)methyl]phenols reacted successfully with 2,4-diamino-6-(alkylthio)pyrimidines to give 5-substituted benzylpyrimidines. The phenolic groups of the products were alkylated in high yield when a nonreactive 6-substituent was present in the pyrimidine ring. 6-(Alkylthio) groups were easily removed with Raney Ni. Trimethoprim (I, R = H, R1 = R2 = MeO) was thus obtained in high yield from its 6-(methylthio) counterpart. The 6-substituted trimethoprim analogs all had low activity as inhibitors of Escherichia coli dihydrofolate reductase and as antibacterial agents.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Hurst, Derek T.’s team published research in Heterocycles in 1977-12-01 | CAS: 38275-56-8

Heterocycles published new progress about pyrimidine halo cyano; cyanopyrimidine; halopyrimidine. 38275-56-8 belongs to class pyrimidines, name is 5-Chloropyrimidine-2-carbonitrile, and the molecular formula is C5H2ClN3, Safety of 5-Chloropyrimidine-2-carbonitrile.

Hurst, Derek T. published the artcileThe synthesis of some halopyrimidines and some routes to cyanopyrimidines, Safety of 5-Chloropyrimidine-2-carbonitrile, the main research area is pyrimidine halo cyano; cyanopyrimidine; halopyrimidine.

Pyrimidines substituted with halo or cyano groups were prepared by several methods. E.g., direct bromination of I gave the bromopyrimidinol II, which with POCl3 gave bromochloropyrimidine III. Chloropyrimidine IV was converted into the cyano derivative V by heating with Me3N in benzene and then in a melt of KCN in AcNH2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Paterson, Thomas’s team published research in Journal of the Chemical Society, Perkin Transactions 17: Organic and Bio-Organic Chemistry in 1972 | CAS: 36075-35-1

Journal of the Chemical Society, Perkin Transactions 17: Organic and Bio-Organic Chemistry published new progress about pyridopyrimidine uracil crotonaldehyde; riboflavin analog. 36075-35-1 belongs to class pyrimidines, name is 7-Methylpyrido[2,3-d]pyrimidine-2,4-diol, and the molecular formula is C8H7N3O2, SDS of cas: 36075-35-1.

Paterson, Thomas published the artcileSpecific enzyme inhibitors in vitamin biosynthesis. I. Synthesis of 8-substituted pyrido[2,3-d]pyrimidines, SDS of cas: 36075-35-1, the main research area is pyridopyrimidine uracil crotonaldehyde; riboflavin analog.

Condensation of 6-(substituted amino)uracils with α,β-unsaturated carbonyl compounds gave 8-substituted pyrido[2,3-d]pyrimidones; e.g., 6-[(2-hydroxyethyl)-amino]uracil (I) reacted with MeCH:CHCHO in 20% HCl at room temperature to give 72% 5,6,7,8-tetrahydro-7-methyl-5,8-(1-oxapropano)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione, which on heating in Ph2O gave 81% 8-(2-hydroxyethyl)-7-methylpyrido[2,3-d]pyrimidine-2,4(3H,8H)-dione (II; R = H, R1 = Me). Substituted pyrido[2,3-d]pyrimidones were also prepared by condensation of 6-(substituted amino)uracils with β-dicarbonyl derivatives; e.g. I with the Na salt of AcCHMeCHO in 85% phosphoric acid gave 47% II (R = Me, R1 = H). PMR studies of II showed that D exchange of protons on C-Me groups at positions 5 and 7 occurred in alk. solution, but protons on a 6-Me group did not exchange; a highly delocalized anionic species was implicated.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Felczak, Krzysztof’s team published research in Collection Symposium Series in 1999 | CAS: 19030-75-2

Collection Symposium Series published new progress about phenylseleno uracil preparation virucide HIV. 19030-75-2 belongs to class pyrimidines, name is 5-N-Propyluracil, and the molecular formula is C7H10N2O2, Synthetic Route of 19030-75-2.

Felczak, Krzysztof published the artcileSynthesis of novel acyclo 6-(phenylseleno)uracils – potential selective anti-HIV agents, Synthetic Route of 19030-75-2, the main research area is phenylseleno uracil preparation virucide HIV.

Starting from 5-propyluracil regioselective syntheses of 1-[(2-hydroxyethoxy)methyl]-6-(phenylseleno)-5-propyluracil, 1-(ethoxymethyl)-6-(phenylseleno)-5-propyluracil and 1-(benzyloxymethyl)-6-(phenylseleno)-5-propyluracil were described. The biol. and pharmacol. activity of the compounds thus prepared was not reported.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pluskota, Donata’s team published research in Synthetic Communications in 1992-11-30 | CAS: 19030-75-2

Synthetic Communications published new progress about methylcytosine; cytosine alkyldimethyl. 19030-75-2 belongs to class pyrimidines, name is 5-N-Propyluracil, and the molecular formula is C7H10N2O2, Related Products of pyrimidines.

Pluskota, Donata published the artcileThe facile synthesis of N(1), N(4)-dimethyl-5-substituted cytosines, Related Products of pyrimidines, the main research area is methylcytosine; cytosine alkyldimethyl.

A facile, high yield synthesis of N(1),N(4)-dimethyl-5-alkylcytosines is described. Thus chlorination of alkyluracils I (R = Me, Et, Pr, Bu) followed by substitution with NaOEt and methylation gave methylpyrimidinones II (R1 = EtO). Substitution of II (R1 = EtO) with MeNH2 gave the title compounds II (R1 = MeNH). This method is an alternative and universal route to N(1),N(4)-methylated cytosines with any 5-substituent.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia