Tag: 200-300

On January 18, 2018, Bartels, Bjoern; Jakob-Roetne, Roland; Limberg, Anja; Neidhart, Werner; Ratni, Hasane; Reutlinger, Michael; Steiner, Sandra published a patent.Safety of 5-Bromo-2,4,6-trichloropyrimidine The title of the patent was Preparation of fused pyrimidine derivatives as γ-secretase inhibitors. And the patent contained the following:

The present invention relates to a compound of formula I wherein R1 is Ph, lower alkyl, C3-6-cycloalkyl, -CH2-C3-6-cycloalkyl or bridged C4-6-cycloalkyl, substituted by one, two or three halogen atoms, or by lower alkyl or lower alkyl substituted by halogen;R2 is a five or six membered heteroaryl group, selected from or wherein R6 is hydrogen, lower alkyl, halogen or lower alkoxy; and R7 is hydrogen, lower alkoxy or halogen; R3 is lower alkyl or lower alkyl substituted by hydroxy: R4 is hydrogen or lower alkyl; R5 is hydrogen or lower alkyl; n is 1 or 2; -( )n- is -CH2- or -CH2CH2- for n being 1 or 2; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Alzheimer’s disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome. Example compound II was prepared by amination of 2-chloro-7-(4-fluorophenyl)-N,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-amine with (1R,5S,8S)-3-(6-methylpyrimidin-4-yl)-3-azabicyclo[3.2.1]octan-8-amine. The invention compounds were evaluated for their γ-secretase inhibitory activity. From the assay, it was determined that compound II exhibited EC50 value of 14 nM. The experimental process involved the reaction of 5-Bromo-2,4,6-trichloropyrimidine(cas: 63931-21-5).Safety of 5-Bromo-2,4,6-trichloropyrimidine

The Article related to pyrimidine preparation gamma secretase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of 5-Bromo-2,4,6-trichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On August 26, 2015, Wang, Nenghui; Xu, Rongzhen; Xie, Meiqiang; Gan, Xiaoxian; Xue, Yinghan published a patent.SDS of cas: 63931-21-5 The title of the patent was Pyrimidine derivative as T790 variation inhibitor. And the patent contained the following:

Title compounds I [wherein A and B independently = N and CH; R1 = C1-C8 linear or branched alkyl or substituted C1-C8 linear or branched alkyl; R2 = C1-C8 linear or branched alkyl, C1-C8 linear or branched alkoxy, etc.; R3 = H, F, Cl, Br, I, etc.; R4 = C1-C8 linear or branched alkyl, substituted C1-C8 linear or branched alkyl, etc.], and their pharmaceutically acceptable salts thereof, were prepared as T790 variation inhibitors useful for treating drug-resistant tumor caused by T790M variation. Thus, the invention compound I [A = B = CH; R1 = i-Pr; R2 = CHF2; R3 = F; R4 = C(O)Me]was prepared from 5-bromo-2,4,6-trichloropyrimidine in a multi-step synthesis. The experimental process involved the reaction of 5-Bromo-2,4,6-trichloropyrimidine(cas: 63931-21-5).SDS of cas: 63931-21-5

The Article related to pyrimidine preparation antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 63931-21-5

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 31, 1986, Mikhaleva, M. A.; Kolesnichenko, G. A.; Rubina, K. I.; Gol’dberg, Yu. Sh.; Savel’ev, V. A.; Leitis, L. Ya.; Shimanskaya, M. V.; Mamaev, V. P. published an article.Quality Control of 5-Phenylpyrimidine-2-carboxylic acid The title of the article was Synthesis of 5-arylpyrimidine-2-carboxylic acids and liquid crystalline properties of their aryl esters. And the article contained the following:

5-Arylpyrimidine-2-carboxylic acids I (R = H, MeO, BuO, R1 = H) were prepared by hydrolysis of 5-aryl-2-cyanopyrimidines and by phase-transfer catalyzed oxidation of 5-aryl-2-styrylpyrimidines. Aryl esters of these acids I (R1 = Ph, substituted Ph) were obtained and their liquid crystalline properties were studied. p-Substituted 5-phenyl-2-pyrimidinecarboxylates do not exhibit mesomorphism, but introduction of a butoxy group in the para position of the pyrimidine attached Ph ring leads to the appearance of nematic properties. In addition, aryl 5-phenylpyrimidincarbonyloxybenzoates are nematic liquid crystals with a thermally stable mesophase at 50-80° during their lifetimes. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).Quality Control of 5-Phenylpyrimidine-2-carboxylic acid

The Article related to aryl arylpyrimidinecarboxylate liquid crystal, pyrimidinecarboxylic acid liquid crystal, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 5-Phenylpyrimidine-2-carboxylic acid

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 8, 2017, Al-Awar, Rima; Zepeda-Velazquez, Carlos Armando; Poda, Gennady; Isaac, Methvin; Uehling, David; Wilson, Brian; Joseph, Babu; Liu, Yong; Subramanian, Pandiaraju; Mamai, Ahmed; Prakesch, Michael; Stille, Julia Kathleen published a patent.Quality Control of 4-(2-Bromopyrimidin-4-yl)morpholine The title of the patent was Preparation of N-aryl heteroarylcarboxamides and arylcarboxamides as inhibitors of WDR5 protein-protein binding. And the patent contained the following:

The application is directed to compounds of formula I and their uses, for example as medicaments for the treatment of diseases, disorders or conditions mediated or treatable by inhibition of binding between WDR5 protein and its binding partners. Compounds of formula I wherein R1 is (un)substituted heterocycloalkyl; R2 is (un)substituted C6-10 aryl and (un)substituted heteroaryl; R3 is (un)substituted C6-10 aryl, (un)substituted heteroaryl and (un)substituted heterocycloalkyl; X1 and X2 are independently CR17 and N; R17 is H, F, C1-6 alkyl and C1-6 fluoroalkyl; A is F, (fluoro)alkyl and (fluoro)alkylene; and pharmaceutically acceptable salts and solvates thereof, are claimed. Example compound II was prepared by multistep procedure (procedure given). The invention compounds were evaluated for their WDR5 protein binding affinity. From the assay, it was determined that compound II exhibited KD value of 0.084 μM. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).Quality Control of 4-(2-Bromopyrimidin-4-yl)morpholine

The Article related to aryl heteroarylcarboxamide arylcarboxamide preparation wdr5 protein binding inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 4-(2-Bromopyrimidin-4-yl)morpholine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 5, 1980, Ishikawa, Fumiyoshi; Ashida, Shinichiro published a patent.Category: pyrimidines The title of the patent was 1,2,3,5-Tetrahydroimidazothienopyrimidin-2-ones and pharmaceutical compositions containing them. And the patent contained the following:

The title compounds I (R, R1 = H, alkyl, Ph, Cl; RR1 = C3-5 alkylene; R2 = H, alkyl) and some isomers in the thiophene ring were prepared Thus 2,4-dichloro-5,6-dimethylthieno[2,3-d]pyrimidine was hydrogenated and cyclized with BrCH2CO2Et to give I (R = R1 = Me, R2 = H, II). II had blood platelet aggregation-inhibiting activity of 84% at 50 mg/kg orally in rats and caused 5 ± 3% decrease in blood pressure at the same dose. The experimental process involved the reaction of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine(cas: 42518-42-3).Category: pyrimidines

The Article related to imidazothienopyrimidinone, platelet aggregation inhibitor imidazothienopyrimidinone, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On August 26, 2015, Wang, Nenghui; Xu, Rongzhen; Xie, Meiqiang; Gan, Xiaoxian; Xue, Yinghan published a patent.Formula: C4BrCl3N2 The title of the patent was Preparation of pyrimidine derivatives as anaplastic lymphoma kinase inhibitors. And the patent contained the following:

The title pyrimidine derivatives I [wherein W = NH; R1 = (un)substituted C1-C8 linear or branched alkyl; R2 = C1-C8 linear or branched alkyl, alkoxy, etc.; or W and R2 form a ring; R3 = H, F, Cl, Br, I, etc.; R4 = S(O2)R5, S(O)R5R6, or P(O)R5R6; R5 and R6 = independently C1-C8 (un)substituted linear or branched alkyl] or pharmaceutically acceptable salts thereof were prepared as anaplastic lymphoma kinase inhibitors for treating cancer, especially non-small cell lung cancer. For example, II was prepared in a multi-step synthesis. The experimental process involved the reaction of 5-Bromo-2,4,6-trichloropyrimidine(cas: 63931-21-5).Formula: C4BrCl3N2

The Article related to preparation pyrimidine anaplastic lymphoma kinase inhibitor treatment cancer human, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C4BrCl3N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 31, 1986, Boehm, R.; Pech, R.; Haubold, Gudrun; Hannig, E. published an article.Computed Properties of 42518-42-3 The title of the article was Thieno compounds. Part 5. Base substituted thieno[2,3-d]pyrimidines. And the article contained the following:

Thienopyrimidines I and II [R = Cl, substituted NH2; R1 = substituted NH2] were prepared by the amination of I or II (R, R1 = Cl). Stepwise amination of I or II (R, R1 = Cl) gave mixed diaminothienopyrimidines. The experimental process involved the reaction of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine(cas: 42518-42-3).Computed Properties of 42518-42-3

The Article related to chlorothienopyrimidine amination, thienopyrimidinamine, aminothienopyrimidine, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 42518-42-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Ruch, Jonas; Aubin, Ariane; Erbland, Guillaume; Fortunato, Audrey; Goddard, Jean-Philippe published an article in 2016, the title of the article was Metal-free arylation of pyrimidines through a photochemical process.Reference of 5-(4-Bromophenyl)pyrimidine And the article contains the following content:

Pyrimidinyl and pyrazinyl radicals were generated under moderate energetic irradiation conditions (UVA), and proved to be prompt to undergo C-C bond formation processes. Hetero-biaryl derivatives were obtained in good to high yields with highly interesting functional group selectivities. Bis hetero-biaryls were also easily accessible leading to original compounds, ready for further transformations. Experiments supporting radical processes were reported. The experimental process involved the reaction of 5-(4-Bromophenyl)pyrimidine(cas: 160377-42-4).Reference of 5-(4-Bromophenyl)pyrimidine

The Article related to pyrimidine arene photoarylation, arylpyrimidine regioselective preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of 5-(4-Bromophenyl)pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On July 1, 2015, Shore, Daniel G. M.; Wasik, Kimberly A.; Lyssikatos, Joseph P.; Estrada, Anthony A. published an article.COA of Formula: C5HCl2F3N2 The title of the article was Minisci alkylations of electron-deficient pyrimidines with alkyl carboxylic acids. And the article contained the following:

A practical method for the Minisci reaction of electron-deficient pyrimidines with carboxylic acids is described. The one-step protocol allows for the alkylation of halo- and trifluoromethyl pyrimidines with a variety of readily available alkyl and (hetero)cycloalkyl carboxylic acids. These conditions permitted the facile synthesis of substituted pyrimidines, which are poised for further elaboration through divergent means. The experimental process involved the reaction of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine(cas: 785777-98-2).COA of Formula: C5HCl2F3N2

The Article related to minisci alkylation electron deficient pyrimidine alkyl carboxylic acid, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C5HCl2F3N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 29, 2007, Han, Cheol Kyu; Yoon, Jeonghyeok; Kim, Nam-Doo; Kim, Jin-Ah published a patent.SDS of cas: 42518-42-3 The title of the patent was Preparation of 5,6-dimethylthieno[2,3-d]pyrimidine derivatives as antiviral agents. And the patent contained the following:

Title compounds represented by the formula I [wherein R1 = 4-morpholinophenyl or 6-morpholinopyridin-3-yl; R2 = 2-, 3- or 4-pyridinyl; and pharmaceutically acceptable salts thereof] were prepared as antiviral agents. For example, reaction of 2,4-dichloro-5,6-dimethylthieno[2,3-d]pyrimidine with 4-(morpholino)aniline (quant.), and followed by reaction with piperazine (15%) and picolinoyl chloride hydrochloride (30%), gave I (R1 = 4-morpholinophenyl, R2 = 2-pyridinyl). The title compounds I showed HCV replicon inhibitory activity with EC50 values of 0.45 – 0.71 μM, and low cytotoxicity. Thus, I and their pharmaceutical compositions are useful for the treatment of hepatitis C. The experimental process involved the reaction of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine(cas: 42518-42-3).SDS of cas: 42518-42-3

The Article related to dimethylthienopyrimidine morpholinophenyl preparation hcv inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 42518-42-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia