Tag: 100-200

In 2018,Wang, Hui-Yan; Shen, Ying; Zhang, Hao; Hei, Yuan-Yuan; Zhao, Hong-Yi; Xin, Minhang; Lu, She-Min; Zhang, San-Qi published 《Discovery of 2-(aminopyrimidin-5-yl)-4-(morpholin-4-yl)-6- substituted triazine as PI3K and BRAF dual inhibitor》.Future Medicinal Chemistry published the findings.Safety of 2,4,6-Trichloropyrimidine The information in the text is summarized as follows:

The discovery and development of novel agents simultaneously targeting PI3K/AKT/mammalian target of rapamycin and Ras/RAF/MEK, two signaling pathways, are urgent to improve the curative effect of kinase inhibitors and overcome acquired resistance. In the present study, 2-(2-aminopyrimidin-5-yl)-4-(morpholin-4-yl)-6-(N-cyclopropyl-N- (1-benzoylpiperidin-4-yl))triazines/pyrimidines were designed as PI3K and BRAF dual inhibitors. The synthesized 20 compounds exhibited potent antiproliferative effects in vitro against HCT116, A375, MCF-7, Colo205, A549 and LOVO cancer cell lines. The tested compounds A6, A7, A9 and A11 remarkably displayed inhibitory activities toward both PI3Kα and BRAFV600E. These results indicated that our design compounds can serve as potent PI3Kα and BRAFV600E dual inhibitors and effective antiproliferative agents, which can be further optimized to discover more potent PI3Kα and BRAFV600E dual inhibitors.2,4,6-Trichloropyrimidine(cas: 3764-01-0Safety of 2,4,6-Trichloropyrimidine) was used in this study.

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Almost all organochlorine compounds are synthesized. It is widely used as intermediates, solvents and pesticides of chemical synthetic products.Safety of 2,4,6-Trichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 1987,Seela, Frank; Steker, Herbert; Driller, Hans Juergen; Bindig, Uwe published 《2-Amino-2′-deoxytubercidin and related pyrrolo[2,3-d]pyrimidinyl-2′-deoxyribofuranosides》.Liebigs Annalen der Chemie published the findings.Category: pyrimidines The information in the text is summarized as follows:

Phase-transfer glycosylation of 2-amino-4-chloro-7H-pyrrolo[2,3-d]pyrimidine with 1-chloro-3,5-di-O-(p-toluoyl)-α-D-erythro-pentofuranose (I) yielded the crystalline nucleoside II in a regio- and diastereoselective reaction. Nucleophilic displacement of the 4-chloro substituent of II or the nonprotected analog opened a route to 2-amino-2′-deoxytubercidin (III) or the thionucleoside IV. The anomers of I were isolated from the glycosylation reaction carried out in the absence of the nucleobase. In the part of experimental materials, we found many familiar compounds, such as 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Category: pyrimidines)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 1985,Seela, Frank; Driller, Hansjuergen; Liman, Ulrich published 《7-Deaza isosters of 2′-deoxyxanthosine and 2′-deoxyspongosine – synthesis via glycosylation of 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine》.Liebigs Annalen der Chemie published the findings.Recommanded Product: 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine The information in the text is summarized as follows:

Glycosylation of 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine with 2-deoxy-3,5-di-O-p-toluoyl-α-D-erythro-pentofuranosyl chloride in DMF in the presence of NaH gave the nucleoside derivative I (R = R1 = Cl; R2 = p-toluoyl) (II) and its α-anomer. II on treatment with NaOMe in MeOH gave I (R = R1 = MeO; R2 = H), which on demethylation with HBr-AcOH in THF gave 7-deaza-2′-deoxyxanthosine (III). II was also converted into 7-deaza-2′-deoxyspongosine (I; R = MeO, R1 = NH2, R2 = H). In the part of experimental materials, we found many familiar compounds, such as 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Recommanded Product: 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own. Recommanded Product: 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidineThey have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 1984,Seela, Frank; Driller, Hansjuergen published 《7-(β-D-Arabinofuranosyl)-2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine – synthesis, selective displacement of halogen, and effect of glyconic protecting groups on the reactivity of the aglycon》.Liebigs Annalen der Chemie published the findings.Application of 90213-66-4 The information in the text is summarized as follows:

Phase-transfer glycosylation of 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine with 2,3,5-tri-O-benzyl-α-D-arabinofuranosyl bromide, followed by column chromatog. gave 67% nucleoside I (R = PhCH2) (II), which on debenzylation with BCl3 gave the title compound I (R = H) (III). Nucleophilic displacement on III resulted in selective substitution of Cl in position 4. Under more vigorous conditions the C-4 as well as the C-2 substituents were replaced. In contrast nucleophilic substitution of II was hindered. In addition to this study using 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine, there are many other studies that have used 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Application of 90213-66-4) was used in this study.

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics. Application of 90213-66-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The author of 《Zwitterionic σ-complexes: their role as intermediates in phosphorylation of aromatics by phosphorus compounds》 were Gololobov, Yu. G.; Onys’ko, P. P.. And the article was published in ACS Symposium Series in 1981. COA of Formula: C5H5N3O3 The author mentioned the following in the article:

Reaction of P(III) compounds with 1,3,5-(O2N)3C6H3 in Me2SO gave σ-complexes I [PR3 = P(OEt)3, PPh(OEt)2, P(OEt)Ph2, P(O)(OEt)2], which were stabilized without a dissociated cation in contrast to ordinary Meisenheimer σ-complexes. 5-Nitropyrimidines do not form stable σ-complexes with (RO)3P or (RO)2P(O)H without bases. II [R = alkyl; R1 = H, MeO, Ph, R2 = H; R1 = H, MeO, R2 = MeO] were prepared only in the presence of Et3N. In addition to this study using 2-Methoxy-5-nitropyrimidine, there are many other studies that have used 2-Methoxy-5-nitropyrimidine(cas: 14001-69-5COA of Formula: C5H5N3O3) was used in this study.

2-Methoxy-5-nitropyrimidine(cas: 14001-69-5) is a member of ether. Friedel Crafts reaction, for example, adds an alkyl or acyl group to aromatic ethers when they react with an alkyl or acyl halide in the presence of a Lewis acid as a catalyst.COA of Formula: C5H5N3O3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Onys’ko, P. P.; Gololobov, Yu. G.; Remennikov, G.; Cherkasov, V. M. published an article in Zhurnal Obshchei Khimii. The title of the article was 《Anion σ-complexes of phosphorus compounds. VII. σ-Complexes of dialkylphosphites with 5-nitropyrimidines》.Formula: C5H5N3O3 The author mentioned the following in the article:

Reaction of I (R = H, MeO, Ph; R1 = H) with (R2O)2P(O)H (R2 = Me, Et) in presence of Et3N gave II (R, R1, R2, as above). Similar reaction of I (R = H, MeO, R1 = MeO) with (R2O)2P(O)H (R2 = Me, Et) gave III via the corresponding intermediate II. In the experiment, the researchers used many compounds, for example, 2-Methoxy-5-nitropyrimidine(cas: 14001-69-5Formula: C5H5N3O3)

2-Methoxy-5-nitropyrimidine(cas: 14001-69-5) is a member of ether. When aromatic ethers are exposed to halogen in the presence or absence of a catalyst, they undergo halogenation, such as bromination.Formula: C5H5N3O3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

COA of Formula: C5H6N2O3On November 20, 1995 ,《Metabolism of ALS inhibitory herbicide Bispyribac-sodium [KIH-2023] in rats》 appeared in Nippon Noyaku Gakkaishi. The author of the article were Fukai, Yasushi; Unai, Tadaaki; Ishikawa, Kanji; Yusa, Yoshio; Wada, Nobuhide; Tezuka, Masakatsu; Okada, Shoji. The article conveys some information:

Absorption, distribution and metabolism of Bispyribac-sodium [sodium 2,6-bis(4,6-dimethoxypyrimidin-2-yloxy)benzoate] or [KIH-2023] in rats orally dosed with 14C-KIH-2023 were investigated. More than 90% of the dosed radioactivity was detected in the excreta within 96 h after dosing. Level of the radioactivity in the blood of male and female rats reached maximum at 2 and 1 h after dosing, resp., and then decreased rapidly to about a half level of maximum (C1/2). The radioactivity of tissues was lower at 96 h after dosing than that at C1/2-time. Most of the radioactivity in the urine, feces, liver, and plasma was detected as unchanged KIH-2023. The major radioactive compounds excreted into the bile were KIH-2023 and its glucuronide. Repeated oral administration of KIH-2023 for 15 days gave similar results from the single oral one in the excretion, tissue distribution and metabolism of 14C-KIH-2023. In the experiment, the researchers used many compounds, for example, 6-Methoxypyrimidine-2,4(1H,3H)-dione(cas: 29458-38-6COA of Formula: C5H6N2O3)

6-Methoxypyrimidine-2,4(1H,3H)-dione(cas: 29458-38-6) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.COA of Formula: C5H6N2O3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood-brain barrier permeability》 was written by Borsari, Chiara; Keles, Erhan; Treyer, Andrea; De Pascale, Martina; Hebeisen, Paul; Hamburger, Matthias; Wymann, Matthias P.. Computed Properties of C4HCl3N2This research focused ontricyclic pyrimido pyrrolooxazine mTOR inhibitor blood brain barrier permeability. The article conveys some information:

Highly selective mTOR inhibitors have been discovered through the exploration of the heteroaromatic ring engaging the binding affinity region in mTOR kinase. Compound 11 showed predicted BBB permeability in a MDCK-MDR1 permeability in vitro assay, being the first pyrimido-pyrrolo-oxazine with potential application in the treatment of neurol. disorders. In addition to this study using 2,4,6-Trichloropyrimidine, there are many other studies that have used 2,4,6-Trichloropyrimidine(cas: 3764-01-0Computed Properties of C4HCl3N2) was used in this study.

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. They are generally not present in crude oils and are typically the result of additives, cleaning solutions or chemicals used for oil recovery.Computed Properties of C4HCl3N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Structure-Guided Optimization Provides a Series of TTK Protein Inhibitors with Potent Antitumor Activity》 was written by Elsner, Jan; Cashion, Dan; Robinson, Dale; Bahmanyar, Sogole; Tehrani, Lida; Fultz, Kimberly E.; Narla, Rama Krishna; Peng, Xiaohui; Tran, Tam; Apuy, Julius; LeBrun, Laurie; Leftheris, Katerina; Boylan, John F.; Zhu, Dan; Riggs, Jennifer R.. Product Details of 90213-66-4This research focused onTTK kinase inhibitor preparation cancer. The article conveys some information:

TTK is an essential spindle assembly checkpoint enzyme in many organisms. It plays a central role in tumor cell proliferation and is aberrantly overexpressed in a wide range of tumor types. We recently reported on a series of potent and selective TTK inhibitors with strong antiproliferative activity in triple neg. breast cancer (TNBC) cell lines (8: TTK IC50 = 3.0 nM; CAL-51 IC50 = 84.0 nM). Inspired by previously described potent tricyclic TTK inhibitor 6 (TTK IC50 = 0.9 nM), we embarked on a structure-enabled design and optimization campaign to identify an improved series with excellent potency, TTK selectivity, solubility, CYP inhibition profile, and in vivo efficacy in a TNBC xenograft model. These efforts culminated in the discovery of 25 (TTK IC50 = 3.0 nM; CAL-51 IC50 = 16.0 nM), which showed significant single-agent efficacy when dosed iv in a TNBC xenograft model without body weight loss. In the experiment, the researchers used many compounds, for example, 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Product Details of 90213-66-4)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics. Product Details of 90213-66-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Extrusion of sulfur from [(acylmethyl)thio]pyrimidinones》 was written by Roth, Barbara; Laube, Renee; Tidwell, Mary Y.; Rauckman, Barbara S.. Category: pyrimidines And the article was included in Journal of Organic Chemistry on August 29 ,1980. The article conveys some information:

Thermally mediated S extrusion from the (phenacylthio)pyrimidinones I (R = H, R1 = Br, H, MeO; R = Me, R1 = Br) occurs rapidly in solution at 125° to yield the (benzoylmetheylene)pyrimidinones II. However, III rearranges via an episulfide intermediate to IV. Adjacent 3- or 5-Me substituents in the pyrimidine ring assist S extrusion. No reaction occurs in the absence of a 2-oxo function or on replacement of it by a 2-amino group. On the other hand, 2-amino-4[(1-methylacetonyl)thio]-6(1H)-pyrimidinone cyclizes very readily to give the thieno pyrimidinone V. 2-(Phenacylthio)-4(3H)-pyrimidinones lose S at about one-seventh the rate of the 4-phenacylthio isomers. No thermally mediated reaction occurs with 2-(acetonylthio)-4-pyrimidinones under the conditions described here. In the part of experimental materials, we found many familiar compounds, such as 2-Methoxy-4-methylpyrimidine(cas: 14001-60-6Category: pyrimidines)

2-Methoxy-4-methylpyrimidine(cas: 14001-60-6) is a member of ether. When aromatic ethers are exposed to halogen in the presence or absence of a catalyst, they undergo halogenation, such as bromination.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia