Category: 67073-96-5

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

Easmon, J. published the artcileThiazolyl and benzothiazolyl hydrazones derived from α-(N)-acetylpyridines and diazines: synthesis, antiproliferative activity and CoMFA studies, SDS of cas: 67073-96-5, the main research area is thiazolyl hydrazone preparation antiproliferative cancer CoMFA; QSAR thiazolyl hydrazone antiproliferative cancer; benzothiazolyl hydrazone antiproliferative cancer CoMFA.

The synthesis of a series of thiazolyl and benzothiazolyl hydrazones derived from α-(N)-acylpyridines, -quinolines, -isoquinolines, -pyridazines, -pyrimidines, and -pyrazines is reported. The stereochem. of these compounds was determined by NMR spectroscopic methods. The antiproliferative activity of the novel compounds was quantified in tissue culture (melanoma, breast carcinoma, colon adenocarcinoma, epitheloid cervix carcinoma, Burkitt’s lymphoma, leukemia, and hydroxyurea sensitive and resistant myelogenous leukemia sublines). All compounds exhibited profound antiproliferative activity, in particular against Burkitt’s lymphoma cells. Out of this series, some were 13-900 times more potent than hydroxyurea and no cross-resistance to hydroxyurea was observed A predictive 3D-QSAR model using the CoMFA approach was established.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 67073-96-5 belongs to class pyrimidines, name is 1-(6-Methylpyrimidin-4-yl)ethanone, and the molecular formula is C7H8N2O, SDS of cas: 67073-96-5.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Easmon, Johnny published the artcileSynthesis, Cytotoxicity, and Antitumor Activity of Copper(II) and Iron(II) Complexes of 4N-Azabicyclo[3.2.2]nonane Thiosemicarbazones Derived from Acyl Diazines, Recommanded Product: 1-(6-Methylpyrimidin-4-yl)ethanone, the main research area is antitumor copper iron thiosemicarbazone complex synthesis Burkitt lymphoma.

A series of thiosemicarbazones (TSCs) (bearing a 4N-azabicyclo[3.2.2]nonane moiety) derived from 3-acylpyridazines, 4-acetylpyrimidines, and 2-acetylpyrazines were synthesized as potential antitumor agents. TSCs exhibited potent cytotoxic activity against human acute lymphoblastic leukemia CCRF-CEM cells (IC = 0.05-0.77 M) and colon adenocarcinoma HT-29 cells (IC = 0.011-2.22 M). Copper II complexes of TSCs showed significant improvement in cytotoxic activity against HT-29 cells (IC50 = 0.004-1.51 μM) by a factor of 3. However, complexation of some TSC ligands with Fe(II) results in lowering of cytotoxic activity by a factor of 7. In clonogenic assays involving human tumor cells of different tumor origins, three of the TSCs and their copper complexes exhibited remarkable cytotoxic activities with mean IC50 values of 6, 0.18, 1, 1, 0.37, and 0.37 nM, resp. In particular, the compounds were highly effective against human colon carcinoma and large and small cell lung carcinoma cells. One of the TSC derivative was evaluated in vivo in nude mice bearing LXFL 529 human large cell lung carcinoma cells. With respect to antitumor activity, application of 30 mg/kg/d resulted in moderate inhibition (42%) of tumor growth. No effect on tumor growth was observed at a dose of 10 mg/kg/d. However, a dose of 40 or 60 mg/kg/d resulted in 50 and 75% death, resp., in the treated mice, indicating the high toxicity of these compounds Using human liver microsomes, one of the TSC compound was rapidly and highly metabolized in vitro. In actual fact, only 2% of the unmetabolized compound could be detected in the incubation medium after 5 min. The IC50 for cell proliferation (0.006-0.022 μM) elicited by these compounds is much lower than that of the inhibition of [14C]cytidine incorporation into DNA (0.18-3.32 μM). These compounds are also non-cell cycle specific agents. Interestingly, three of these compounds were potent inducers of apoptosis in Burkitt’s lymphoma cells.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 67073-96-5 belongs to class pyrimidines, name is 1-(6-Methylpyrimidin-4-yl)ethanone, and the molecular formula is C7H8N2O, Recommanded Product: 1-(6-Methylpyrimidin-4-yl)ethanone.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Sakamoto, Takao published the artcileStudies on pyrimidine derivatives. XVI. Site selectivity in the homolytic substitution of simple pyrimidines, Recommanded Product: 1-(6-Methylpyrimidin-4-yl)ethanone, the main research area is substitution homolytic pyrimidine; acylation pyrimidine homolytic; hydroxymethylation pyrimidine homolytic; oxidation methylpyrimindine; crosscoupling reaction methylpyrimidine; coupling reaction methylpyrimidine cross; amidation methylpyrimidine; ethoxycarbonylation methylpyrimidine; ketone pyrimidine; amide pyrimidine.

Pyrimidines in which both the 2- and 4-positions are free showed site selectivity in their reactions with radicals generated in redox systems. Thus treating 6-phenyl- (I), 6-methylpyrimidine, and 5,6,7,8-tetrahydroquinazoline with radicals, e.g. RC•O, R2NC•O, EtO2C•, •CH2OH, gave predominantly the 4-substituted products. Only the reaction of I with Me2NC•O gave any 2-substituted products.

Chemical & Pharmaceutical Bulletin published new progress about Cross-coupling reaction. 67073-96-5 belongs to class pyrimidines, name is 1-(6-Methylpyrimidin-4-yl)ethanone, and the molecular formula is C7H8N2O, Recommanded Product: 1-(6-Methylpyrimidin-4-yl)ethanone.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Brumfield, Martha A. published the artcileTwo triplets mediating intramolecular photochemical abstraction of hydrogen by nitrogen in 4-acyl-6-alkylpyrimidines, Recommanded Product: 1-(6-Methylpyrimidin-4-yl)ethanone, the main research area is photocyclization acylalkylpyrimidine; intramol photochem hydrogen abstraction acylalkylpyrimidine; triplet state hydrogen abstraction acylaklylpyrimidine; pyrimidine acylalkyl triplet photochem.

Direct irradiation with λ >340 nm of 4-acyl-6-alkylpyrimidines I (R = Me) and II (R = CH2CH2CHMe2) or their triplet sensitization by aromatic ketones leads to an nπ* triplet (ET ∼70-71 kcal/mol). In I (R = Me) this state is responsible for hydrogen abstraction from the C(4) side chain and isomerization to cyclopropanol III. Ketone II (R = CH2CH2CHMe2) does not fragment under either of these direct or sensitized conditions. However, triplet sensitization of II (R = CH2CH2CHMe2) by acetone (ET ∼79-82 kcal/mol) or direct irradiation of II (R = CH2CH2CHMe2) through Vycor, λ > 200 nm, leads to hydrogen abstraction, cleavage of the C(6) side chain, and formation of II (R = Me) in a reaction occurring from an upper nπ* triplet (ET ∼79-84 kcal/mol). Ketone I (R = CH2CH2CHMe2) yields mainly IV and, depending upon conditions, a small amount of I (R = Me) or III; the minor products arise by a novel monophotonic pathway.

Journal of the American Chemical Society published new progress about Photoabstraction reaction, intramolecular photoabstraction. 67073-96-5 belongs to class pyrimidines, name is 1-(6-Methylpyrimidin-4-yl)ethanone, and the molecular formula is C7H8N2O, Recommanded Product: 1-(6-Methylpyrimidin-4-yl)ethanone.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Rao, C. Janakiram published the artcileSubstituent Effects on Photochemical Hydrogen Abstraction in 2-Acylpyridines, 2-Acylpyrazines, and 4-Acylpyrimidines, Quality Control of 67073-96-5, the main research area is photochem hydrogen abstraction acylheterocycle substituent effect; ketone photochem hydrogen abstraction.

Stern-Volmer quenching of the photochem. of I indicates that N- and O-abstraction are quenched at different rates . When I is sensitized with triplet sensitizers of increasing ET, N-abstraction increases . These data indicate that N- and O-abstraction in I take place from distinguishable triplet states. Survey of Φp’s of ring-substituted nitrogen-containing heteroaryl ketones (e.g. II; R= H,Me,CN) demonstrates the effect of substitution on the competition between N- and O-abstraction . For methyl- and dicyano-substituted ketones, the results can be understood simply in terms of shifts in ET of the nπ* and ππ* states of the heterocycle. The photochem. of all these ketones requires consideration of interactions among three triplet states.

Journal of Organic Chemistry published new progress about Heterocyclic compounds, nitrogen Role: RCT (Reactant), RACT (Reactant or Reagent). 67073-96-5 belongs to class pyrimidines, name is 1-(6-Methylpyrimidin-4-yl)ethanone, and the molecular formula is C7H8N2O, Quality Control of 67073-96-5.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia