Day: November 2, 2022

On May 10, 2022, Zhang, Xuejun; Chang, Shaohua; Lei, Sijun; Ding, Xiaohua; Chen, Haomin; Jing, Zhenzhong; Yang, Chengbing; Liu, Lifei; Yang, Jun; Li, Lie published a patent.Name: 2-Chloro-5-isopropylpyrimidine The title of the patent was Preparation of nitrogen-substituted heterocyclic thiophenes and their uses in preparation of a medicament for the treatment of LPAR-related diseases. And the patent contained the following:

The present invention relates to the preparation of nitrogen-substituted heterocyclic thiophenes and their uses in preparation of a medicament for the treatment of LPAR-related diseases. In particular, the nitrogen-substituted heterocyclic thiophene compound I (wherein, R1 = -H, -CN, halogen, -Z-Ra, the following groups (un)substituted by Rb: C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkylamino, C1-6 alkoxy; Z = single bond, -O-, -S- or -CO-; Ra is = C1-6 alkyl, C1-6 alkyl substituted by halogen, amino, C1-3 alkylamino; Rb = -CN, halogen, C1-6 alkyl, C1-6 alkoxy groups; R2 = -H, -CN, halogen, -Y-Rd, the following groups (un)substituted by Re: C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkylamino, C1-6 alkoxy; Y = single bond or -O-, -S-; Rd = C1-6 alkyl, C1-6 alkyl group substituted by halogen; Re = -CN, halogen, C1-6 alkyl, C1-6 alkoxy groups). Further, ( X1, X2, X3 = C or N, and X1, X2, X3 = not N at the same time; Rg is selected from H, F, Cl, methyl; L1 = single bond, -N(R3)- or -O-; L2 = single bond, -O-, C1-6 alkylene (un)substituted by C1-3 alkyl, unsubstituted or cyclopropyl substituted by C1-3 alkyl; R3 = -H, C1-3 alkyl; R4 = -H, -CN, halogen, the following groups (un)substituted by Rh: C1-6 alkyl, C3-8 cycloalkyl; and Rh = -H, halogen, C1-6 alkyl, C1-6 alkyl substituted by halogen, C1-6 alkoxy substituted by halogen groups) was prepared The compound of the present invention has good antagonism to LPAR1, and has good antagonism to LPAR3. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Name: 2-Chloro-5-isopropylpyrimidine

The Article related to nitrogen substituted heterocyclic thiophene preparation lpar antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: 2-Chloro-5-isopropylpyrimidine

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

Borodkin, Gennady I.; Elanov, Innokenty R.; Gatilov, Yury V.; Shubin, Vyacheslav G. published an article in 2016, the title of the article was Promotional effect of ionic liquids in electrophilic fluorination of methylated uracils.Related Products of 626-48-2 And the article contains the following content:

A novel efficient protocol has been developed for fluorination of methylated uracils involving a stoichiometric amount of ionic liquid (IL) in alcs. The fluorination of 6-methyluracil and 1,3,6-trimethyluracil has been carried out using the electrophilic fluorinating reagent Selectfluor (F-TEDA-BF4) in MeOH and EtOH solvents with the formation of 5-fluoro-6-methyluracil, 5-fluoro-1,3,6-trimethyluracil as well as α-fluoromethoxy- and α-fluoroethoxy ethers of difluorodihydrouracils as the main products. The use of a stoichiometric amount of ionic liquid as an additive results in acceleration of the reaction. It has been found that the effect of the anion of the IL on the rate of the reaction is more pronounced compared to that of the cation, the effectiveness of the anions decreasing in the following order: [HSO4-] > [OTf-] ~[NTf2-] > [BF4-] > [PF6-]. The influence of metal carbonates on the yields of fluorouracils has also been evaluated. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Related Products of 626-48-2

The Article related to fluorouracil preparation green chem, electrophilic fluorination ionic liquid, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 626-48-2

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

On March 28, 2019, Chen, Chen published a patent.Computed Properties of 175357-98-9 The title of the patent was Preparation of cyclic iminopyrimidine derivatives as B-Raf V600E kinase inhibitors. And the patent contained the following:

The invention relates to cyclic iminopyrimidine compounds and their bicyclic derivatives of formula I and their preparation, useful in treating proliferation disorders such as cancer or tumors or for diseases or disorders related to the dysregulation of kinase such as, but not limited to B-Raf V600E kinase. Compounds of formula I are claimed, in which X1, X2, X3, Y1, Y2, and Y3 are each independently N and (un)substituted CH; Z1 is O, S, and (un)substituted NH and CH2; Z2 is bond and NH and derivatives; m = 0-3, n = 1-3; R1-R3 are each independently H, halo, CN, NO2, (un)substituted C1-6 alkyl, etc.; R4 is H and C1-6 alkyl; or pharmaceutically acceptable salts, solvates, or isotopic derivatives thereof. Example compound II was prepared via a multistep process (procedure given). Invention compounds were evaluated for their B-Raf V600E kinase inhibitory activity. From the assay, it was determined that II exhibited growth inhibition of 50% (GI50) at <100 nM. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Computed Properties of 175357-98-9

The Article related to cyclic iminopyrimidine dihydroimidazoquinazoline preparation kinase inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 175357-98-9

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 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 December 31, 2015, Meshcheryakova, S. A.; Kataev, V. A.; Fattakhova, I. Ya.; Nikolaeva, K. V.; Bulgakov, A. K. published an article.Category: pyrimidines The title of the article was Synthesis and Antimicrobial Activity of Thietanylpyrimidin-2,4(1H,3H)-Dione Acetanilides and Acetylhydrazones. And the article contained the following:

Alkylation of 6-methyl-1-(thietan-3-yl)pyrimidine-2,4(1H,3H)-dione with chloroacetanilides yielded N-acetanilide derivatives Interaction of 2-4-methyl-2,6-dioxo-3-thietan-3-yl-3,6-dihydropyrimidin-1(2H)-acetohydrazide with carbonyl compounds was used to synthesize arylaldehyde and ketone N-acetylhydrazones. The antimicrobial and antifungal activities of the compounds synthesized here were studied. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Category: pyrimidines

The Article related to thietanylpyrimidindione acetanilide acetylhydrazone preparation antimicrobial agent, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: pyrimidines

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 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