Tag: M.W:100-200

Application In Synthesis of 2,6-Dichloropurine. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Study of the N7 Regioselective Glycosylation of 6-Chloropurine and 2,6-Dichloropurine with Tin and Titanium Tetrachloride.

6-Chloropurine and 2,6-dichloropurine were regioselectively glycosylated at position 7 to give the corresponding peracetylated N7-nucleosides, which can be suitable for other purine transformations. In this work, we study the distribution of N7/N9-isomers produced via the Vorbruggen method under different conditions, using an N-trimethylsilylated purine derivative and SnCl4 or TiCl4 as a catalyst. The main effort is devoted to reversing the disadvantageous predominant selectivity of most glycosylation reactions at the N9 position and thus to determining conditions that maximize the regioselectivity of glycosylation toward the desired N7-isomer.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 6-Hydroxy-2-methylpyrimidin-4(3H)-one( cas:1194-22-5 ) is researched.Recommanded Product: 6-Hydroxy-2-methylpyrimidin-4(3H)-one.Chen, Lei-xiang; Deng, Sheng-song; Guan, Qiu-xiang; Gu, Lei-ming published the article 《Synthesis and process research of 4,6-dichloro-2-methylpyrimidine》 about this compound( cas:1194-22-5 ) in Anhui Huagong. Keywords: acetamidine hydrochloride dimethyl malonate synthesis. Let’s learn more about this compound (cas:1194-22-5).

4,6-Dichloro-2-methylpyrimidine is an important intermediate of synthetic anticancer drug dasatinib. 4,6-Dichloro-2-methylpyrimidine was synthesized from acetamidine hydrochloride and di-Me malonate via the cyclization and chlorination with phosphorus oxychloride. The optimal conditions of synthesis of 4,6-dihydroxy-2-methyipyrimidine were investigated by orthogonal test. They were: n(acetamidine hydrochloride)/n (sodium methoxide)=1:3.4, in methanol at 20°C for 4h, the yield of 4, 6-dihydroxy-2-methylpyrimidine was 85.76%. The optimal conditions of chlorination with phosphorus oxychloride were investigated by orthogonal test. They were: n (N,N-diethyl-Benzenamine)/n (4,6-dihydroxy-2-methylpyrimidine)=2:1, in phosphorus oxychloride at 105°C for 4 h, the yield of 4,6-dichloro-2-methylpyrimidine was 69.55%, the yield of two-steps was 59.65%.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Formula: C5H2Cl2N4. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about NMR studies of new heterocycles tethered to purine moieties with anticancer activity. Author is Fernandez-Saez, Nerea; Campos, Joaquin M.; Camacho, Maria Encarnacion; Carrion, Maria Dora.

The synthesis and biol. evaluation of a novel family of purine derivatives linked to six-membered heterocyclic moieties, which were designed and evaluated as anticancer agents, are described. The structures of these new compounds have been determined by 1H and 13C NMR and mass spectrometry. Some of them have been studied more in detail in order to corroborate their skeleton by using two-dimensional techniques.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Safety of 2,6-Dichloropurine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Synthesis and fluorescent properties of N(9)-alkylated 2-amino-6-triazolylpurines and 7-deazapurines. Author is Sisulins, Andrejs; Bucevieius, Jonas; Tseng, Yu-Ting; Novosjolova, Irina; Traskovskis, Kaspars; Bizdena, Erika; Chang, Huan-Tsung; Tumkevieius, Sigitas; Turks, Maris.

The synthesis of novel fluorescent N(9)-alkylated 2-amino-6-triazolylpurine and 7-deazapurine derivatives is described. A new C(2)-regioselectivity in the nucleophilic aromatic substitution reactions of 9-alkylated-2,6-diazidopurines and 7-deazapurines with secondary amines has been disclosed. The obtained intermediates, 9-alkylated-2-amino-6-azido-(7-deaza)purines, were transformed into the title compounds by CuAAC reaction. The designed compounds belong to the push-pull systems and possess promising fluorescence properties with quantum yields in the range from 28% to 60% in acetonitrile solution Due to electron-withdrawing properties of purine and 7-deazapurine heterocycles, which were addnl. extended by triazole moieties, the compounds with electron-donating groups showed intramol. charge transfer character (ICT/TICT) of the excited states which was proved by solvatochromic dynamics and supported by DFT calculations In the 7-deazapurine series this led to increased fluorescence quantum yield (74%) in THF solution The compounds exhibit low cytotoxicity and as such are useful for the cell labeling studies in the future.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 6-Hydroxy-2-methylpyrimidin-4(3H)-one, is researched, Molecular C5H6N2O2, CAS is 1194-22-5, about Synthesis, molecular modeling and biological activity of methyl and thiomethyl substituted pyrimidines as corticotropin releasing hormone type 1 antagonists, the main research direction is methyl thiomethyl substituted pyrimidine preparation mol modeling biol activity; corticotropin releasing hormone antagonist methyl thiomethyl substituted pyrimidine.Formula: C5H6N2O2.

Four small, targeted libraries of differentially substituted amino pyrimidines were synthesized in moderate to good yields. Excellent regiochem. was observed for substitution at C2/C4 with selectivity >50 : 1 noted. All analogs were screened for their ability to interact with CRH1 and CRH2 receptors. In all instances only poor agonistic and/or antagonistic behavior was noted at CRH2. However, several compounds were potent and selective CRH1 antagonists, most notably one compound showed Ki = 39 nM. Addnl. we have utilized these data and that recently reported by others to refine our original CRH1 pharmacophore (J. Med. Chem., 1999, 42, 2351-2357).

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Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Product Details of 5451-40-1. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Discovery of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives as novel tubulin polymerization inhibitors for treatment of cancer. Author is Zhang, Qiangsheng; Hu, Xi; Wan, Guoquan; Wang, Jia; Li, Lu; Wu, Xiuli; Liu, Zhihao; Yu, Luoting.

A new series of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives I [R1 = H, i-Pr, Et2CH, cyclopentyl, tetrahydropyran-2-yl; R2 = H, Cl, 4-F3COC6H4, 3-(morpholin-4-yl)phenyl, 6-(4-methylpiperazin-1-yl)pyridin-3-yl, etc.] was designed, synthesized and demonstrated to act as tubulin polymerization inhibitors. These new derivatives showed significant antitumor activities, among which compound I [R1 = cyclopentyl; R2 = Cl (II)] was found to be the most potent compound, with IC50 values ranging from 44.5 to 135.5 nM against seven colorectal carcinoma (CRC) cell lines. Remarkably, compound II exhibited no activity against other potential targets, such as 420 kinases and EZH2. Besides, compound II inhibited tubulin polymerization, arrested the cell cycle at the G2/M phase and induced apoptosis in CRC cells. Furthermore, compound II suppressed tumor growth in the HCT116 xenograft model without inducing notable major organ-related toxicity, suggesting that this compound could be used as a promising lead compound for the development of new antitumor agents.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Kapadiya, Khushal M.; Khunt, Ranjan C. published the article 《Discovery of Hybrid Purine-quinoline Molecules and Their Cytotoxic Evaluation》. Keywords: purine quinoline hybrid mol NSCLC cytotoxicity.They researched the compound: 2,6-Dichloropurine( cas:5451-40-1 ).COA of Formula: C5H2Cl2N4. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:5451-40-1) here.

Apart from the “”hit drugs””, there are many others being studied for their potent activity against several hostilities. To date, anticancer research has been exploited on the inherent versatility and active core skeleton of the compounds Literature suggests that nitrogen rich mols. are most active and found in their potent cancer activity. Purine-based compounds such as olomoucine and roscovitine, which contain other heterobicyclic ring systems, are useful for the cell proliferation inhibitors in the treatment of many types of cancer. We put forward the novel purine based compounds, aryl amino-quinoline-purine by a two-step procedure. In the first step, nitrogen rich mol. was synthesized by the coupling of 2,6- dichloropurine with 3-aminoquinoline in an acidic reaction conditions at the C-6 position of purine. Aryl amines were introduced at the C-2 position by acid catalyst and using polar solvent at comparatively higher reaction conditions to furnish the desired products. Stereochem. aspect was introduced for the identification of attachment of 3-aminoquinoline at the C-2/C-6 position of purine and it was concluded by the spectral anal. (HMBC spectrum). The spectral data revealed that the first chloro-amine coupling was directed at the C-6 position rather than C-2 and the second chloro-amine coupling by various aryl amines were directed at the C-2 position. The applications of synthesized compounds were identified by their cytotoxic study against NCI-60 cell-lines. Out of nine selected mols. by NCI, 5a has shown promising response in a single dose study and GI50 value, 7.57μM indicated that it has 7.57% lethality over HOP-92 cell-line (non-small cell lung cancer panel). Two straightforward novelties were introduced, first stereochem. identification for chloro-amine coupling in purine either at the C-2 or C-6 position on the basis of HMBC spectrum. And a second type of uniqueness was to identify better anti-cancer agents out of synthesized scaffolds. Overall study shows that compound 5a is a novel therapeutic agent after modification for the treatment of non-small cell lung and it satisfied determined threshold growth inhibition criteria at a single dose level.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: Ethyl 3-bromo-2-oxopropanoate, is researched, Molecular C5H7BrO3, CAS is 70-23-5, about Wood ash biocatalyst as a novel green catalyst and its application for the synthesis of benzochromene derivatives.Application In Synthesis of Ethyl 3-bromo-2-oxopropanoate.

This study investigates the catalytic activity of wood ash as a heterogeneous catalyst for the synthesis of benzochromene derivatives I (R = Me, 4-methoxyphenyl, Ph, Et, 4-methylphenyl; R1 = 4-methoxyphenyl, C(O)OC2H5, 4-methylphenyl). Several wood ash catalysts, comprising calcium- and potassium-rich carbonates, were prepared from different natural resources under various combustion temperatures The prepared catalysts were characterized by Fourier transform IR, SEM, energy dispersive X-ray anal., transmission electron microscopy, and X-ray diffraction techniques. Catalytic efficiency of the resultant catalysts was tested in the synthesis of benzochromene derivatives I. The exptl. studies clarified that the catalyst prepared at 850 °C could efficiently expedite the formation of three-component synthesis of benzochromene derivatives I in water at 80 °C with high yields. Indeed, alkali, alk. metal, and metal oxides such as Al2O3, SiO2, MgO, CaO, and Fe2O3, are widely utilized as both catalyst and catalyst support in the heterogeneous catalytic processes. The prepared wood ash catalysts (possessing metal oxides, e.g., CuO, Al2O3, SiO2, and CaO) could effectively prompt the electrophilic activity of the carbonyl groups during the nucleophilic attack intermediate, enhancing the efficiency of the reactions.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Prevention and rescue of cardiac dysfunction by methanocarba adenosine monophosphonate derivatives, the main research direction is cardiac dysfunction methanocarba adenosine monophosphonate derivative; Adenine nucleoside phosphonate; Cardiac function; Heart failures; Purinergic receptors.Related Products of 5451-40-1.

Abstract: Accumulating evidence supports a therapeutic role of purinergic signaling in cardiac diseases. Previously, efficacy of systemically infused MRS2339, a charged methanocarba derivative of 2-Cl-adenosine monophosphate, was demonstrated in animal models of heart failure. We now test the hypothesis that an uncharged adenine nucleoside phosphonate, suitable as an oral agent with a hydrolysis-resistant phospho moiety, can prevent the development of cardiac dysfunction in a post-infarction ischemic or pressure overload-induced heart failure model in mice. The diester-masked uncharged phosphonate MRS2978 was efficacious in preventing cardiac dysfunction with improved LV fractional shortening when administered orally at the onset of ischemic or pressure overload-induced heart failure. MRS2925, the charged, unmasked MRS2978 analog, prevented heart dysfunction when infused s.c. but not by oral gavage. When administered orally or systemically, MRS2978 but not MRS2925 could also rescue established cardiac dysfunction in both ischemic and pressure overload heart failure models. The diester-masked phosphate MRS4074 was highly efficacious at preventing the development of dysfunction as well as in rescuing pressure overload-induced and ischemic heart failure. MRS2978 was orally bioavailable (57-75%) giving rise to MRS2925 as a minor metabolite in vivo, tested in rats. The data are consistent with a novel therapeutic role of adenine nucleoside phosphonates in systolic heart failure.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Synthetic Route of C5H2Cl2N4. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Structure-Based Optimization of Quinazolines as Cruzain and TbrCATL Inhibitors. Author is Barbosa da Silva, Elany; Rocha, Debora A.; Fortes, Isadora S.; Yang, Wenqian; Monti, Ludovica; Siqueira-Neto, Jair L.; Caffrey, Conor R.; McKerrow, James; Andrade, Saulo F.; Ferreira, Rafaela S..

The cysteine proteases, cruzain and TbrCATL (rhodesain), are therapeutic targets for Chagas disease and Human African Trypanosomiasis, resp. Among the known inhibitors for these proteases, N4-benzyl-N2-phenylquinazoline-2,4-diamine (1a I [R1 = phenyl; R2 = benzyl] in this study), as a competitive cruzain inhibitor (Ki = 1.4μM) was described. The synthesis and biol. evaluation of 22 analogs I [R1 = Ph, 4-OH-Ph, 2-pyridyl; R2 = benzyl, Ph, 3-Cl-Ph, etc] of I [R1 = phenyl; R2 = benzyl], containing modifications in the quinazoline core, and in the substituents in positions 2 and 4 of this ring was described. The analogs I demonstrate low micromolar inhibition of the target proteases and cidal activity against Trypanosoma cruzi with up to two log selectivity indexes in counterscreens with myoblasts. Fourteen compounds were active against Trypanosoma brucei at low to mid micromolar concentrations During the optimization of I [R1 = phenyl; R2 = benzyl], structure-based design and prediction of physicochem. properties were employed to maintain potency against the enzymes while removing colloidal aggregator characteristics observed for some mols. in this series.

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Oxazolidine – Wikipedia,
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