Pyrimidines

On June 30, 2005, Freyne, Eddy Jean Edgard; Willems, Marc; Storck, Pierre Henri; Poncelet, Virginie Sophie; Van Emelen, Kristof; Buijnsters, Peter Jacobus Johannes Antonius; Embrechts, Werner Constant Johan; Perera, Timothy Pietro Suren published a patent.Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine The title of the patent was Pyrido- and pyrimidopyrimidine derivatives as antiproliferative agents. And the patent contained the following:

The present invention concerns pyrido- and pyrimidopyrimidine macrolide derivatives One example compound prepared was I. Reactions are given for preparation of a number of intermediates and other derivatives similar to I. Pharmacol. data include in vitro inhibition of EGF receptors and serum starved proliferation assay on ovarian carcinoma SKOV3 cells. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

The Article related to pyridopyrimidine pyrimidopyrimidine derivative preparation antiproliferative agent, Heterocyclic Compounds (More Than One Hetero Atom): Eight- and Higher-Membered Rings and other aspects.Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 20, 2003, Neya, Masahiro; Sawada, Akihiko; Ohne, Kazuhiko; Abe, Yoshito; Mizutani, Tsuyoshi; Ishibashi, Naoki; Inoue, Makoto published a patent.COA of Formula: C10H7BrN2 The title of the patent was Preparation of 2-(thiophenyl)thiopyran-1,1-dioxides as MMP or TNF-α inhibitors. And the patent contained the following:

Title compounds I [wherein R1 = (un)substituted Ph, naphthyl, bicyclic heterocyclyl, alkenyl, or alkynyl; R2 = CO2H or protected CO2H; or a salt thereof] were prepared as matrix metalloproteinase (MMP) or tumor necrosis factor α (TNF-α) inhibitors. For example, coupling of 2-(trimethylsilyl)ethyl (S)-[2-(5-bromothiophen-2-yl)-1,1-dioxo-3,4,5,6-tetrahydro-2H-thiopyran-2-yl]acetate and 2-(4′-cyano-4-biphenylyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane followed by deesterification gave II. Five compounds of the invention were tested for gelatinolytic activity against human MMP-9 and displayed inhibitory activity with IC50 values ranging from 1.37 nM to 16.0 nM. Thus, I are useful for treating and/or preventing diseases mediated by MMP or TNF-α (no data). The experimental process involved the reaction of 5-(4-Bromophenyl)pyrimidine(cas: 160377-42-4).COA of Formula: C10H7BrN2

The Article related to thiophenyl thiopyrandioxide preparation mmp tnf inhibitor, Heterocyclic Compounds (One Hetero Atom): Thiopyrans and Areno- and Diarenothiopyrans and other aspects.COA of Formula: C10H7BrN2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On December 1, 2019, Drozd, Ksenia V.; Manin, Alex N.; Perlovich, German L. published an article.HPLC of Formula: 626-48-2 The title of the article was Comparative analysis of experimental methods for determining thermodynamic parameters of formation of multi-component molecular crystals: Benefits and limitations. And the article contained the following:

In this work, we have studied the processes of dissolution of 4-aminobenzoic acid (PABA) two-component crystals with 6-methyluracil (6-MeUr), pyrazinamide (PyrAm) and emoxypine (EMX) in the pH 7.4 phosphate buffer. The thermodn. functions of cocrystal/salt formation have been estimated from the cocrystal/salt solubility and the corresponding solubility of the pure compounds at various temperatures By analyzing the investigated binary systems, we have compared the accuracy of different exptl. methods in evaluating the thermodn. stability of two PABA cocrystals and one salt: the method of phase solubility diagrams and the cocrystal solubility method. A qual. evaluation of the comparative stability of the cocrystals and salt has been conducted by the competitive reactions method. The lowest value of the Gibbs energy of formation has been found in the PABA cocrystal with 6-MeUr. The fact that the PABA salt with EMX has the highest absolute value of the Gibbs energy of formation is associated with proton transfer. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).HPLC of Formula: 626-48-2

The Article related to multi component mol crystal solubility thermodn stability, Phase Equilibriums, Chemical Equilibriums, and Solutions: Phase Equilibriums, Solubility and other aspects.HPLC of Formula: 626-48-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Okafor, Charles O.; Steenberg, Marie L.; Buckley, Joseph P. published an article in 1977, the title of the article was Studies in the heterocyclic series. XIII. New CNS-depressants derived from 1,9-diazaphenoxazine and two isomeric triazaphenothiazine ring systems.Application In Synthesis of 5-Bromo-2,4,6-trichloropyrimidine And the article contains the following content:

Triazaphenothiazines I (R = NH2, H, SMe, OMe; R1 = NH2, Me, Cl, OH, OMe) and II (R = H, NH2, Cl; R1 = NH2, OH, Cl; R2 = MeO, Cl) were prepared in 78-93% yield. Reaction of 2-amino-3-mercapto-6-picoline with 2-amino-5-bromo-4-chloro-6-methylpyrimidine in the presence of H2SO4 and Na2SO3 gave 77% I (R = NH2, R1 = Me). All I and II showed appreciable CNS depressant activities comparable with the activity of chlorpromazine when tested in mice and rats; I (R = H, R1 = NH2) and II (R = R1 = Cl, R2 = MeO) were the most promising. All I and II decreased motor activity and rate of respiration within 30 min and body temperature was decreased by 0.5-1.9° compared to 0.8° with chlorpromazine. The experimental process involved the reaction of 5-Bromo-2,4,6-trichloropyrimidine(cas: 63931-21-5).Application In Synthesis of 5-Bromo-2,4,6-trichloropyrimidine

The Article related to depressant triazaphenothiazine, triazaphenothiazine, phenothiazine triaza, Heterocyclic Compounds (More Than One Hetero Atom): Thiazines (Including Cephalosporins) and other aspects.Application In Synthesis of 5-Bromo-2,4,6-trichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Qiu, Ran; Sun, Jiamu; Zhang, Xin; Zhao, Wenbo; Qin, Zhen; Luo, Hai published an article in 2016, the title of the article was Isomer differentiation through supramolecular self-assembly in microdroplets of milliseconds life-time.Product Details of 626-48-2 And the article contains the following content:

Supramol. recognition of thymine (or its analogs) with various central cations can form magic number clusters. Dual nano-ESI via theta tip emitters was used to online synthesize clusters. Even thermodynamically unstable clusters can be detected by MS thanks to the very short life-time ( approx. ms) of the generated microdroplets. By recording characteristic cluster distributions, isomers can be clearly differentiated in a novel bottom-up way. Theor. calculations were performed to explain the MS results. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Product Details of 626-48-2

The Article related to isomer differentiation supramol selfassembly microdroplet millisecond lifetime, Physical Organic Chemistry: Degradation Reactions, Including Mass Spectral Fragmentation and other aspects.Product Details of 626-48-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 2, 2017, Kubica, Dominika; Molchanov, Sergey; Gryff-Keller, Adam published an article.Reference of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione The title of the article was Solvation of Uracil and Its Derivatives by DMSO: A DFT-Supported 1H NMR and 13C NMR Study. And the article contained the following:

1H NMR and 13C NMR spectra of uracil, thymine, 5-hydroxymethyluracil, 5,6-dihydrouracil, and 5,6-dihydrothymine in DMSO-d6 solutions have been measured. Addnl., mol. structures as well as NMR parameters of these compounds and their various solvates have been calculated using DFT B3LYP/6-311++G(2d,p) PCM(DMSO) method. The anal. of the chem. shift data for these compounds has shown that, indeed, in DMSO solutions they occur as equilibrium mixtures of free mols. and solvates in which solute and solvent mols. are joined by NH···O or OH···O hydrogen bonds. The populations of particular species present in the solutions have been estimated Moreover, it has been found that 5,6-dihydrothymine exists in DMSO solution preferentially in conformation with the Me group occupying the pseudoequatorial position. This finding is based on the mol. energy calculations and remains in full agreement with the interpretation of NMR data and theor. calculations of NMR parameters. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Reference of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione

The Article related to uracil thymine hydroxymethyluracil dihydrouracil dihydrothymine solvation dmso nmr dft, Phase Equilibriums, Chemical Equilibriums, and Solutions: Phase Equilibriums, Solubility and other aspects.Reference of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Sahin, Saliha; Karkar, Buesra published an article in 2019, the title of the article was The antioxidant properties of the chestnut bee pollen extract and its preventive action against oxidatively induced damage in DNA bases.Quality Control of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione And the article contains the following content:

Chestnut bee pollen has potential nutritional and medicinal effects and is an important natural bee product. This study focused on the investigation of the antioxidant capacity and DNA damage inhibition ability of chestnut bee pollen (CBP) from Bursa (Turkey). The phenolic compounds (rosmarinic acid, vitexin, hyperoside, pinocembrin, trans-chalcone, apigenin, protocatechuic, and galangin) and carotenoids in CBPE were determined by HPLC-DAD (high-performance liquid chromatog.-diode array detection). Addnl., the protective ability of CBPE against DNA damage by oxidation was investigated. In this study, it was determined that CBPE has a high total phenolic compound content, and the antioxidant capacity of CBPE inhibits DNA oxidation (34% reduction of DNA damage in Fenton reaction media). This study could reveal new information regarding the use of CBPE as a protective agent for DNA in the future. Practical applications : Phenolic compounds and carotenoids prevent some diseases because of their important biol. activities. One of the potential food sources chestnut bee pollen contains sugar, carbohydrates, amino acids, proteins, lipids, vitamins, hormones, enzymes, and flavonoids. Chestnut bee pollen, which has protective activity against DNA oxidation, could be an excellent potential source of a protective agent against some degenerative diseases through future applications. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Quality Control of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione

The Article related to antioxidant property chestnut bee pollen extract, dna oxidation, fenton, antioxidant, carotenoid, phenolic content, Food and Feed Chemistry: Additives, Sweeteners, Flavorings, Condiments, and Confectionery and other aspects.Quality Control of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On December 20, 2012, Kawamura, Madoka; Kobashi, Yohei; Matsuda, Daisuke; Shiozawa, Fumiyasu; Suga, Yoichiro; Fusegi, Keiko; Kakinuma, Hiroyuki; Otake, Norikazu published a patent.Name: 2-Chloro-5-isopropylpyrimidine The title of the patent was Preparation of azaspiroalkane compounds as GPR119 agonists. And the patent contained the following:

Title compounds I [p = 0-2; q = 1 or 2; ring A = benzene ring or 6-membered heteroaryl; R11-R13 = independently H, halo, carbamoyl, etc.; X = -O- or -NR3-; R3 = H or alkyl; Y = alkanediyl; R2 = alkyl (optionally substituted with cycloalkyl or aryl), alkylsulfonyl, alkylcarbonyl, etc.; or pharmaceutically acceptable salts thereof], useful for the treatment of diabetes, were prepared For example, treatment of tert-Bu 2-(methoxymethylidene)-7-azaspiro[3.5]nonane-7-carboxylate (preparation given) with CF3CO2H/water, reaction with NaH/triethyl phosphonoacetate, hydrogenation, reduction using LiAlH4, reaction with 4-cyano-3-fluorophenol in the presence of N,N,N’,N’-tetramethylazodicarbamide, hydrolysis, and EDCI-mediated amidation with 2-aminoethanol afforded compound II. In GPR119 agonist activity test, EC50 of II was 9 nM. Pharmaceutical compositions comprising I are disclosed. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Name: 2-Chloro-5-isopropylpyrimidine

The Article related to azaspiroalkane preparation gpr119 agonist, diabetes treatment azaspiroalkane gpr119 agonist, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Name: 2-Chloro-5-isopropylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 4, 2014, Kawamura, Madoka; Shiozawa, Fumiyasu; Matsuda, Daisuke; Kakinuma, Hiroyuki; Otake, Kenichi published a patent.Related Products of 596114-50-0 The title of the patent was Preparation of azaspiroalkane compounds as GPR119 agonists. And the patent contained the following:

Title compounds I [spiro moiety represented by Q1 in I is optionally substituted with alkyl or fluoro, may combine with cycloalkane to form a spiro ring, and may form a bridged ring with alkanediyl or alkenediyl; p = 0-3; q = 1-3; n1 = 0-2; n2 = 0-2 such as n1 + n2 = 1 or 2; ring A = benzene ring or 6-membered heteroaryl; R11-R13 = independently H, halo, carbamoyl, etc.; X = -O-, -S- or -NRx-; Rx = H or alkyl; Y = alkanediyl; R2 = alkyl (optionally substituted with cycloalkyl), haloalkyl, cycloalkyl, etc.; or pharmaceutically acceptable salts thereof], useful for the treatment of diabetes, were prepared For example, treatment of tert-Bu 2-(methoxymethylidene)-7-azaspiro[3.5]nonane-7-carboxylate (preparation given) with CF3CO2H/water, reaction with NaH/triethyl phosphonoacetate, hydrogenation, reduction, reaction with 4-cyano-3-fluorophenol in the presence of N,N,N’,N’-tetramethylazodicarbamide, hydrolysis, and EDCI-mediated amidation with 2-aminoethanol afforded compound II. In GPR119 agonist activity test, EC50 of II was 9 nM. Pharmaceutical compositions comprising I are disclosed. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Related Products of 596114-50-0

The Article related to azaspiroalkane preparation gpr119 agonist, diabetes treatment azaspiroalkane gpr119 agonist, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Related Products of 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On June 30, 2014, Kawamura, Madoka; Shiozawa, Fumiyasu; Kakinuma, Hiroyuki; Otake, Kenichi; Matsuda, Daisuke; Kobashi, Yohei; Suga, Yoichiro; Fusegi, Keiko published a patent.Quality Control of 2-Chloro-5-isopropylpyrimidine The title of the patent was Preparation of azaspiroalkane compounds as GPR119 agonists. And the patent contained the following:

The title compounds [I; p = 0-2; q = 1 or 2; ring A = benzene ring or 6-membered heteroaryl; R11-R13 = independently H, halo, carbamoyl, etc.; X = -O- or -NR3-; R3 = H or alkyl; Y = alkanediyl; R2 = alkyl (optionally substituted with cycloalkyl or aryl), alkylsulfonyl, alkylcarbonyl, etc.; or pharmaceutically acceptable salts thereof], useful for the treatment of diabetes, were prepared For example, treatment of tert-Bu 2-(methoxymethylidene)-7-azaspiro[3.5]nonane-7-carboxylate (preparation given) with CF3CO2H/water, reaction with NaH/triethyl phosphonoacetate, hydrogenation, reduction using LiAlH4, reaction with 4-cyano-3-fluorophenol in the presence of N,N,N’,N’-tetramethylazodicarbamide, hydrolysis, and EDCI-mediated amidation with 2-aminoethanol afforded compound (II). In GPR119 agonist activity test, EC50 of II was 9 nM. Pharmaceutical compositions comprising I are disclosed. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Quality Control of 2-Chloro-5-isopropylpyrimidine

The Article related to azaspiroalkane preparation gpr119 agonist, diabetes treatment azaspiroalkane gpr119 agonist, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Quality Control of 2-Chloro-5-isopropylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia