Tag: 100-200

Time-Efficient Synthesis of Pyrido[2,3-d]pyrimidinones via α-Oxoketenes was written by Castillo, Juan-Carlos;Quiroga, Jairo;Rodriguez, Jean;Coquerel, Yoann. And the article was included in European Journal of Organic Chemistry in 2016.Product Details of 54030-56-7 This article mentions the following:

α-Oxoketene reactive intermediates generated in situ by microwave-assisted Wolff rearrangement of 2-diazo-1,3-dicarbonyl compounds have been found to react with 6-aminopyrimidine derivatives as 1,3-C,N-bis-nucleophiles to yield pyrido[2,3-d]pyrimidinones and related compounds amenable to further functionalization. Thus, e.g., Friedel-Crafts/imination cascade reaction of 3-diazoacetylacetone with 6-amino-1,3-dimethyluracil under microwave radiation afforded pyridopyrimidinone I (98%). In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7Product Details of 54030-56-7).

6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Product Details of 54030-56-7

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Assembly of Silver(I) Two- and Three-Dimensional Coordination Networks with Complementary Tridentate Heteroaryl Ethynide Ligands was written by Zhao, Liang;Mak, Thomas C. W.. And the article was included in Inorganic Chemistry in 2009.Recommanded Product: 2-Ethynylpyrimidine This article mentions the following:

Three pairs of complementary N heteroaryl ligands [2,6-(CC)₂-py and 2-CC-pym; 2,5-(CC)₂-py and 2-CC-pyz; 3,5-(CC)₂-py and 5-CC-pym (py = pyridine, pyz = pyrazine, pym = pyrimidine)], wherein a ring N atom in one is interchanged with a C atom bearing an ethynyl substituent in the other, were used to generate seven Ag(I) complexes (1–7), in which Ag infinite chains and two-dimensional coordination networks bridged by heteroaryl ethynide ligands were obtained as pre-programmed. The relative positions and bonding preference between the ethynide group and ring N atom act as controlling factors to produce various structural building units for the formation of multidimensional coordination networks. The fusion of CC⊃Ag_n (n = 3, 4) building units yields multinuclear Ag aggregates in 1–6 whose nuclearities range from seven to twelve. The crystal structure of 7 displays a honeycomb layer composed of Ag₄ baskets alternately linked by pyrimidinyl-5-ethynide ligands. Complex 1 features an infinite chain composed of an alternate arrangement of twist-boat H₂O hexamers and bridging Ag atoms. In the experiment, the researchers used many compounds, for example, 2-Ethynylpyrimidine (cas: 37972-24-0Recommanded Product: 2-Ethynylpyrimidine).

2-Ethynylpyrimidine (cas: 37972-24-0) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Recommanded Product: 2-Ethynylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine reactions. XXII. Relative reactivities of corresponding chloro-, bromo-, and iodopyrimidines in aminolysis was written by Brown, Desmond J.;Arantz, B. W.. And the article was included in Journal of the Chemical Society [Section] C: Organic in 1971.SDS of cas: 16879-39-3 This article mentions the following:

Times of half completion of aminolysis of 2-halo- (I), 5-bromo-2-halo- (II), 2-halo-4,6-dimethyl- (III), and 4-halo-2,6-dimethylpyrimidines (IV) by isopentylamine (V) and 1,4-dimethylpentylamine (VI) are reported. For aminolysis of I with V the relative reactivities were Br > Cl, and with VI, Br ≫ Cl; for aminolysis of II with VI, Br > Cl; for aminolysis of III with V, Br > Cl ≫ I, and with IV, Br ∼ I ≫ Cl; for aminolysis of IV with V or VI Br ≫ I > Cl, but the greatest difference in rate was only about 3-fold. Eight (isopentylamino)- or (1,4-dimethylpentyl)aminopyrimidines derived from these reactions were characterized, and the preparations of 2,5-dibromo-, 1,2-dihydro-5-iodo-2-oxo-, 2-chloro-5-iodo-, and 4-bromo-2,6-dimethylpyrimidine were described. Ionization constants and uv spectra for solutions in cyclohexane are given. In the experiment, the researchers used many compounds, for example, 2-Bromo-4,6-dimethylpyrimidine (cas: 16879-39-3SDS of cas: 16879-39-3).

2-Bromo-4,6-dimethylpyrimidine (cas: 16879-39-3) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.SDS of cas: 16879-39-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

H₁-antihistaminic and antimuscarinic effects of 2- and 4-[benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds was written by Maggiali, C.;Morini, Giovanni;Mossini, F.;Morini, Giuseppina;Barocelli, E.;Impicciatore, M.. And the article was included in Farmaco, Edizione Scientifica in 1988.Name: 4-Chloro-2-methoxypyrimidine This article mentions the following:

Fourteen 2- (I) and 4-[benzyl-(2-dimethylaminoethyl)amino]pyrimdidines (II) (in both cases R, R¹ and R³ = OMe or H; R² = SMe, Cl, or H) were prepared In tests on the isolated guinea pig ileum, I were more potent than II as antihistaminics, but the only compound which was a pure H₁-antihistaminic was II (R = R¹ = OMe; R² = R³ = H), which had a potency similar to that of tonzylamine. In the same test system, the only compound to display a specific antimuscarinic activity (though of low potency) was II (R = R³ = H; R¹ = OMe; R² = Sme). Structure-activity relations are discussed in detail. In the experiment, the researchers used many compounds, for example, 4-Chloro-2-methoxypyrimidine (cas: 51421-99-9Name: 4-Chloro-2-methoxypyrimidine).

4-Chloro-2-methoxypyrimidine (cas: 51421-99-9) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Name: 4-Chloro-2-methoxypyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Discovery of Molidustat (BAY 85-3934): A Small-Molecule Oral HIF-Prolyl Hydroxylase (HIF-PH) Inhibitor for the Treatment of Renal Anemia was written by Beck, Hartmut;Jeske, Mario;Thede, Kai;Stoll, Friederike;Flamme, Ingo;Akbaba, Metin;Ergueden, Jens-Kerim;Karig, Gunter;Keldenich, Joerg;Oehme, Felix;Militzer, Hans-Christian;Hartung, Ingo V.;Thuss, Uwe. And the article was included in ChemMedChem in 2018.Computed Properties of C8H10ClN3O This article mentions the following:

Small-mol. inhibitors of hypoxia-inducible factor prolyl hydroxylases (HIF-PHs) are currently under clin. development as novel treatment options for chronic kidney disease (CKD) associated anemia. Inhibition of HIF-PH mimics hypoxia and leads to increased erythropoietin (EPO) expression and subsequently increased erythropoiesis. Herein the authors describe the discovery, synthesis, structure-activity relationship (SAR), and proposed binding mode of novel 2,4-diheteroaryl-1,2-dihydro-3H-pyrazol-3-ones as orally bioavailable HIF-PH inhibitors for the treatment of anemia. High-throughput screening of the authors’ corporate compound library identified BAY-908 as a promising hit. The lead optimization program then resulted in the identification of molidustat (BAY 85-3934), a novel small-mol. oral HIF-PH inhibitor. Molidustat is currently being investigated in clin. phase III trials as molidustat sodium for the treatment of anemia in patients with CKD. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Computed Properties of C8H10ClN3O).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Computed Properties of C8H10ClN3O

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Clean synthesis and antibacterial activities of spiro[pyrimido[4,5-b]-quinoline-5,5′-pyrrolo[2,3-d]pyrimidine]-pentaones was written by Ghahremanzadeh, Ramin;Azimi, Seyyedeh Cobra;Gholami, Nader;Bazgir, Ayoob. And the article was included in Chemical & Pharmaceutical Bulletin in 2008.Name: 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one This article mentions the following:

A simple, clean and efficient method for the synthesis of spiro[pyrimido[4,5-b]quinoline-5,5′-pyrrolo[2,3-d]pyrimidine]-pentaone derivatives by condensation reaction of 6-amino-uracils and isatins in aqueous media is reported. These products were evaluated in vitro for their antibacterial activities. In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7Name: 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one).

6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Name: 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Novel B-ring modified combretastatin analogs: syntheses and antineoplastic activity was written by Hatanaka, Toshihiro;Fujita, Koichi;Ohsumi, Koji;Nakagawa, Ryusuke;Fukuda, Toshihiro;Nihei, Yukio;Suga, Yasuyo;Akiyama, Yukio;Tsuji, Takashi. And the article was included in Bioorganic & Medicinal Chemistry Letters in 1998.Application of 90905-32-1 This article mentions the following:

A series of B-ring modified combretastatin analogs were synthesized and their inhibitory activity against microtubule assembly, cytotoxic activity against Colon 26 adenocarcinoma cancer cell line were evaluated. Among these, pyridone derivative (I) showed strong antimitotic activity and cytotoxicity, along with excellent water-solubility In the experiment, the researchers used many compounds, for example, 2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1Application of 90905-32-1).

2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Application of 90905-32-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Discovery and SAR studies of novel 2-anilinopyrimidine-based selective inhibitors against triple-negative breast cancer cell line MDA-MB-468 was written by Jo, Jeyun;Kim, Sou Hyun;Kim, Heegyu;Jeong, Myeonggyo;Kwak, Jae-Hwan;Taek Han, Young;Jeong, Jee-Yeong;Jung, Young-Suk;Yun, Hwayoung. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2019.Computed Properties of C8H10ClN3O This article mentions the following:

Triple-neg. breast cancers (TNBCs) are characterized as an invasive and intractable subtype of breast cancers. Overexpression of epidermal growth factor receptor (EGFR) has been considered to be an important target for TNBC therapy, but efficacies of EGFR inhibitors in clin. trials are elusive. In this study, novel series of 2-anilinopyrimidines were synthesized in an effort to identify selective inhibitors against an EGFR-overexpressing TNBC cell line. Biol. evaluation demonstrated that compounds I and II, with a 4-methylpiperidine group and a high ClogP value, exhibited good potency and selectivity for the TNBC cell line. This study has provided evidence to support further development of 2-anilinopyrimidine-based TNBC selective inhibitors and investigation of the targets of compounds I and II. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Computed Properties of C8H10ClN3O).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Computed Properties of C8H10ClN3O

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia