Month: November 2022

Newmark, Philip published the artcileSubstrate specificity of the dihydrouracil dehydrogenase and uridine phosphorylase of rat liver, Recommanded Product: 5-N-Propyluracil, the main research area is LIVER/metabolism; NUCLEASES/metabolism; PHOSPHORYLASES/metabolism.

Studies were conducted to determine whether unnatural pyrimidines (e.g. 5-fluorouracil) which are able to inhibit the degradation of uracil and thymine in a complete rat-liver-enzyme system were the only ones reduced by dihydrouracil dehydrogenase (I), and whether reduction of the inhibiting pyrimidines by the I was a prerequisite for inhibition. Thymine reduction was slower than that of uracil. The relative rates of reduction of 5-halagenouracils were F > Cl > Br > I, 5-iodouracil being slower than uracil and 5-fluoro-uracil faster. I reduced 2-thiouracil, 6-azamacil, and 5-aminouracil relatively slowly. 5-Hydroxyuracil and 5alkyluracils were not reduced, but were effective inhibitors of uracil and thymine degradation. Neither cytosine nor 6-methyluracil acted in either capacity.

Biochimica et Biophysica Acta published new progress about LIVER/metabolism; NUCLEASES/metabolism; PHOSPHORYLASES/metabolism. 19030-75-2 belongs to class pyrimidines, name is 5-N-Propyluracil, and the molecular formula is C7H10N2O2, Recommanded Product: 5-N-Propyluracil.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Sakamoto, Takao published the artcileSelectivity on the homolytic acylation of pyrimidine derivatives, Safety of 1-(6-Methylpyrimidin-4-yl)ethanone, the main research area is homolytic regioselective acylation pyrimidine.

Pyrimidines I [R, R1 = H, Ph; H, Me; RR1 = (CH2)4] were treated with acetyl radical, generated from R2CHO (R2 = Me) FeSO4, tert-BuOOH and H2SO4, to give 25-45% the 4-acetyl derivatives II (R2 = Ac). No 2-acetyl derivatives were formed. Similar reactions using I (R = H, R1 = Ph) and R2CHO (R2 = Et, iso-Pr, Ph) gave 28-50% corresponding II.

Heterocycles published new progress about homolytic regioselective acylation pyrimidine. 67073-96-5 belongs to class pyrimidines, name is 1-(6-Methylpyrimidin-4-yl)ethanone, and the molecular formula is C7H8N2O, Safety of 1-(6-Methylpyrimidin-4-yl)ethanone.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Stoner, Eric J. published the artcileSynthesis of HIV Protease Inhibitor ABT-378 (Lopinavir), HPLC of Formula: 192725-50-1, the main research area is ABT378 lopinavir large scale synthesis; oxopyrimidineacetate large scale synthesis.

A large-scale process for the synthesis of HIV protease inhibitor candidate ABT-378 was developed which utilizes an intermediate common to the synthesis of ritonavir, Abbott’s first generation compound The synthesis relies on the sequential acylation of this intermediate which is carried through as a mixture of diastereomers until the penultimate step. A synthesis of (S)-tetrahydro-α-(1-methylethyl)-2-oxo-1(2H)-pyrimidineacetate, derived from L-valine, is also reported.

Organic Process Research & Development published new progress about ABT378 lopinavir large scale synthesis; oxopyrimidineacetate large scale synthesis. 192725-50-1 belongs to class pyrimidines, name is (S)-3-Methyl-2-(2-oxotetrahydropyrimidin-1(2H)-yl)butanoic acid, and the molecular formula is C9H16N2O3, HPLC of Formula: 192725-50-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Gacek, M. published the artcileMetahalones, a new class of metaphase inhibitors, Formula: C5H5ClN2S, the main research area is metahalone metaphase inhibitor; liver metaphase arrest metahalone; pyrimidine halogenated metaphase inhibition.

A total of 31 halogenated pyrimidine derivatives were tested for metaphase-arresting activity 6 h after addition to monolayer cultures of human liver cells (Chang strain). O-substituted derivatives were inactive, whereas N-substituted derivatives were active. The metaphase-inhibiting activity depended largely on the structure and substituent groups of the compounds tested. The name metahalones is suggested for this class of inhibitors: meta from metaphase, hal from halogen, and one because the activity was associated with the one-form of the 2-hydroxy group.

FEBS Letters published new progress about Liver. 38275-42-2 belongs to class pyrimidines, name is 5-Chloro-2-(methylthio)pyrimidine, and the molecular formula is C5H5ClN2S, Formula: C5H5ClN2S.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Barrett, Harold W. published the artcileSynthetic pyrimidines as inhibitors of uracil and thymine degradation by rat-liver supernatant, Related Products of pyrimidines, the main research area is CATALYSIS; EXPERIMENTAL LAB STUDY; LIVER FUNCTION; METABOLISM; NADP; OXIDOREDUCTASES; PHARMACOLOGY; PYRIMIDINES; RATS; THYMINE; URACIL.

The ability of a number of synthetic pyrimidines to inhibit degradation of uracil and thymine by rat-tissue supernatants was examined Among 9 tissues tested, only liver preparations showed significant pyrimidine-degrading activity, and among 46 compounds tested, only 5-substituted uracils, analogs of thymine, showed appreciable inhibition of pyrimidine degradation. Despite their structure, all active compounds were more effective inhibitors of uracil than of thymine degradation; similarly, uracil and thymine showed reciprocal inhibition, but thymine was considerably more effective. It was concluded that inhibition occurred only during the initial reductive step in pyrimidine degradation, that reduction of both uracil and thymine was catalyzed by the same enzyme (dihydrouracil dehydrogenase), and that inhibition resulted from substrate competition for the active site on the enzyme.

Biochimica et Biophysica Acta, Specialized Section on Nucleic Acids and Related Subjects published new progress about Liver. 19030-75-2 belongs to class pyrimidines, name is 5-N-Propyluracil, and the molecular formula is C7H10N2O2, Related Products of pyrimidines.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Wagner, Gabor published the artcile4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as high-affinity non-imidazole histamine H3 receptor agonists with in vivo central nervous system activity, Product Details of C7H10ClN3, the main research area is aminoazetidinylpyrimidine amine preparation human histamine H3 receptor agonist.

Despite the high diversity of histamine H3 receptor (H3R) antagonist/inverse agonist structures, partial or full H3R agonists have typically been imidazole derivatives An inhouse screening campaign intriguingly afforded the non-imidazole 4-(3-azetidin-1-yl)pyrimidin-2-amine I (R1 = CHMe2, R2 = Me) (II) as partial H3R agonist. Here, the design, synthesis and structure-activity relationships of analogs of II are described. This series yields several non-imidazole full agonists with potencies varying with the alkyl substitution pattern on the basic amine following the in vitro evaluation of H3R agonism using a CRE-luciferase reporter gene assay. The key compound VUF16839, I (R1 = H, R2 = n-Pr) (III), combines nanomolar on-target activity (pKi = 8.5, pEC50 = 9.5) with weak activity on CYP enzymes and good metabolic stability. The proposed H3R binding mode of III indicates key interactions similar to those attained by histamine. In vivo evaluation of III in a social recognition test in mice, revealed an amnesic effect at 5 mg/kg i.p. The excellent in vitro and in vivo pharmacol. profile and the non-imidazole structure of III make it a promising tool compound in H3R research.

Journal of Medicinal Chemistry published new progress about Amnesia. 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.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Looper, Ryan E. published the artcileSynthesis of the putative structure of 7-deoxycylindrospermopsin: C7 oxygenation is not required for the inhibition of protein synthesis, Formula: C4HBr3N2, the main research area is deoxycylindrospermopsin C7 preparation oxygenation protein synthesis.

The cyanobacterial metabolite 7-deoxycylindrospermopsin I was synthesized and its natural occurrence confirmed by HPLC. Structural anal. and protein-inhibition studies show that the uracil unit does not appear to adopt the unconventional tautomeric structure (see scheme), as previously thought, and that oxygenation at C7 is not required for the inhibition of protein biosynthesis.

Angewandte Chemie, International Edition published new progress about Tautomers. 36847-11-7 belongs to class pyrimidines, name is 2,4,6-Tribromopyrimidine, and the molecular formula is C4HBr3N2, Formula: C4HBr3N2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Foldenyi, R. published the artcileSelectivity in oxidation reactions of methylthio-substituted pyrimidines and triazines, Formula: C5H5ClN2S, the main research area is methylthiopyrimidine oxidation; pyrimidine methylthio oxidation; triazine methylthio oxidation.

It was found during the oxidation of methylthio-substituted pyrimidines and 1,3,5-triazines that pyrimidinesulfones were obtained in better yield than triazinesulfones because the oxidation is influenced by the structure and substitution of the heterocycles and it could not be selectively stopped at this level. Depending on pH and solvent, the methylsulfonyl and the formed methylsulfonium groups can rapidly take part in nucleophilic substitution reactions resulting in hydroxylated and methoxylated triazines and pyrimidines. These reactions may be utilized in such processes where the methylthio substituted heterocycles are formed as byproducts. After oxidation, the nucleophilic substitution leads to the desired products.

Hungarian Journal of Industrial Chemistry published new progress about Oxidation. 38275-42-2 belongs to class pyrimidines, name is 5-Chloro-2-(methylthio)pyrimidine, and the molecular formula is C5H5ClN2S, Formula: C5H5ClN2S.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Benneche, Tore published the artcileSelective oxidations and syntheses of α-halomethylthiopyrimidines, Recommanded Product: 5-Chloro-2-(methylthio)pyrimidine, the main research area is pyrimidine halomethylthio preparation oxidation; oxidation selective halomethylthiopyrimidine; sulfide pyrimidinyl selective oxidation; sulfoxide halomethyl pyrimidinyl.

The molybdenum peroxide complex, MoO3.(Me2N)3PO.H2O was a useful reagent for the oxidation of sulfides to sulfones, in particular for the oxidation of a 2-[(iodomethyl)thio]pyrimidine to its sulfone. The α-chloro analog has also prepared by m-ClC6H4C(O)OOH (I) oxidation α-Halo sulfoxides were prepared selectively by I oxidations Synthesis of the α-halo sulfides are described.

Chemica Scripta published new progress about Oxidation. 38275-42-2 belongs to class pyrimidines, name is 5-Chloro-2-(methylthio)pyrimidine, and the molecular formula is C5H5ClN2S, Recommanded Product: 5-Chloro-2-(methylthio)pyrimidine.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Prakash, Anjanappa published the artcileEfficient indoles and anilines syntheses employing tert-butyl sulfinamide as ammonia surrogate, HPLC of Formula: 38275-56-8, the main research area is aniline sulfinamide tert butyl preparation; aryl halide amination tert butyl sulfinamide palladium catalyst; indole preparation bromophenylethyne cross coupling tert butyl sulfinamide palladium.

Tert-Bu sulfinamide is an ammonia equivalent for the palladium-catalyzed amination of aryl bromides and aryl chlorides. Using these amine derivatives, it has been observed that substituted indoles and anilines with sensitive functional groups can be readily prepared This surrogate has also been used for the synthesis of indoles from (2-bromophenyl)ethynes using palladium-catalyzed cross coupling reaction as the key step.

Tetrahedron Letters published new progress about Amination. 38275-56-8 belongs to class pyrimidines, name is 5-Chloropyrimidine-2-carbonitrile, and the molecular formula is C5H2ClN3, HPLC of Formula: 38275-56-8.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia