Pyrimidines

On January 2, 2020, Kanouni, Toufike; Arnold, Lee D.; Kaldor, Stephen W.; Murphy, Eric A.; Tyhonas, John published a patent.Recommanded Product: 785777-98-2 The title of the patent was Inhibitors of cyclin-dependent kinases. And the patent contained the following:

Provided herein are inhibitors of cyclin-dependent kinases (CDKs), pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases. The experimental process involved the reaction of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine(cas: 785777-98-2).Recommanded Product: 785777-98-2

The Article related to cyclin dependent kinase cdk12 inhibitor preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 785777-98-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On May 31, 2019, Bartels, Bjoern; Cook, Xinlan Aloise Ford; Ratni, Hasane; Reutlinger, Michael; Vifian, Walter published a patent.Product Details of 63931-21-5 The title of the patent was Preparation of pyrimidine derivatives as Aβ42 inhibitor. And the patent contained the following:

The invention provides pyrimidine compounds with formula I as Aβ24 inhibitor. Compounds of formula I wherein each R1 is independently H and halo; R2 is H and methyl; R3 is five membered heteroaryl group; n is 1, 2 and 3; X is N and C; A is is a (un)substitued bicyclo[1.1.1]pentane or (un)stituted bicyclo[2.2.2]octane; and a pharmaceutically acceptable salt thereof; are claimed. Example compound II was prepared by N-alkylation of 3-(4-methylimidazol-1-yl)bicyclo[1.1.1]pentan-1-amine with 2-chloro-7-(4-fluorophenyl)-N,5,5-trimethyl-6H-pyrrolo[2,3-d]pyrimidin-4-amine. The compounds of formula I were evaluated for their Aβ24 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 of 0.032 μM. The experimental process involved the reaction of 5-Bromo-2,4,6-trichloropyrimidine(cas: 63931-21-5).Product Details of 63931-21-5

The Article related to pyrimidine derivative preparation protein inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Product Details of 63931-21-5

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On May 11, 2017, Gaufreteau, Delphine; Kolczewski, Sabine; Plancher, Jean-Marc; Stoll, Theodor published a patent.Related Products of 1209459-32-4 The title of the patent was Preparation of 6-(pyrimidin-2-yl)indolin-2-one derivatives useful in the treatment of CNS-related disorders. And the patent contained the following:

The invention is concerned with indolin-2-one derivatives of formula I that are useful in the treatment of CNS-related diseases. Compounds of formula I wherein A is Ph, pyrazinyl, pyridazinyl, pyrimidinyl, pyridinyl, etc.; R1 and R2 are independently H, lower acyl. cycloalkyl, lower alkyl, etc.; R1R2 may be taken together to form morpholinyl, oxopyrrolidinyl, substituted piperidinyl, etc.; R3 is H and lower alkyl; and pharmaceutically acceptable salts, racemic mixtures, enantiomers, optical isomer and stereoisomers thereof, are claimed. Example compound II was prepared by N-arylation of 3,3-dimethyl-6-(2-methylpyrimidin-5-yl)indolin-2-one with 4-(6-bromopyrazin-2-yl)morpholine. The invention compounds were evaluated for their ENT1 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 0.0390 μM. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).Related Products of 1209459-32-4

The Article related to pyrimidinylindolinone preparation treatment cns disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 1209459-32-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On August 31, 2017, Raskildina, G. Z.; Valiev, V. F.; Ozden, I. V.; Meshcheryakova, S. A.; Spirikhin, L. V.; Zlotskii, S. S. published an article.Recommanded Product: 6-Methylpyrimidine-2,4(1H,3H)-dione The title of the article was Synthesis of pyrimidine-2,4(1H,3H)-dione derivatives containing N-alkyl substituents. And the article contained the following:

6-Methyluracil derivatives containing a gem-dichlorocyclopropane and a 1,3-dioxolane fragments were synthesized for the first time. The condensation of 6-methyluracil with chloromethyl derivatives gives a mixture of N1- and N3-monosubstituted products, and the profound N-alkylation of this compound provides disubstituted uracils. The structure of the synthesized compounds was studied by H1 and 13C NMR spectroscopy and their relative antioxidant activity was evaluated by luminol-dependent chemiluminescence measurements. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Recommanded Product: 6-Methylpyrimidine-2,4(1H,3H)-dione

The Article related to pyrimidinedione alkyl derivative preparation antioxidant, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 6-Methylpyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 15, 2018, Blake, James F.; Burgess, Laurence E.; Chicarelli, Mark Joseph; Christensen, James Gail; Fell, Jay Bradford; Fischer, John P.; Gaudino, John J.; Hicken, Erik James; Hinklin, Ronald Jay; Lee, Matthew Randolf; Marx, Matthew Arnold; Mejia, Macedonio J.; Rodriguez, Martha E.; Savechenkov, Pavel; Tang, Tony P.; Vigers, Guy P.A.; Zecca, Henry J. published a patent.Category: pyrimidines The title of the patent was Preparation of substituted pyrido[3,4-d]pyrimidine compounds as KRas G12C inhibitors. And the patent contained the following:

The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds I [X = (un)substituted 4-12 membered saturated or partially saturated monocyclic, bridged or spirocyclic ring; Y = a bond, O, S or NR5; R1 = C(O)C(R)(= or )C(R’)p, or SO2C(R)(= or )C(R’)p; R2 = H, alkyl, hydroxyalkyl, etc.; Z = alkylene; R3 = (independently) alkyl, oxo, or haloalkyl; L = a bond, C(O), or alkylene; R4 = H, cycloalkyl, heterocyclyl, etc.; R5 = (independently) H or alkyl; R = absent, H, or alkyl; R’ = (independently) H, alkyl, alkylaminylalkyl, etc.; p = 0-1; m = 0-2] that irreversibly inhibit the activity of KRas G12C, to pharmaceutical compositions comprising the compounds and methods of use therefor. Over 400 compounds I were prepared E.g., a multi-step synthesis of (2S)-II, starting from (S)-tert-Bu 2-(hydroxymethyl)pyrrolidine-1-carboxylate, was described. Exemplified compounds I were tested in the KRas G12C modification assay, and for inhibition of KRas G12C-dependent cell growth (data given). The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Category: pyrimidines

The Article related to pyridopyrimidine preparation kras g12c inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On October 23, 1997, Bridges, Alexander James; Denny, William Alexander; Dobrusin, Ellen Myra; Doherty, Annette Marian; Fry, David W.; Mcnamara, Dennis Joseph; Showalter, Howard Daniel Hollis; Smaill, Jeffrey B.; Zhou, Hairong published a patent.Reference of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine The title of the patent was Preparation of N-quinazolinylacrylamides and analogs as tyrosine kinase inhibitors. And the patent contained the following:

Title compounds [I; R = (CHR6)pR9; R1R2 = CH:CR7CR8:CH, CH:CR7CR8:N, CH:CR7N:CH, etc.; R6 = H or alkyl; 1 of R7,R8 = Z1Z2R10 and the other = OR4, SR4, NHR3; R3,R4 = (un)substituted alkyl, heterocyclylalkyl, etc.; R9 = (un)substituted Ph; R10 = CR11:CHR5, CCR5, CR11:C:CHR5; R5 = H, halo, alkyl, Ph, etc.; R11 = H, halo, alkyl; Z1 = bond, O, (alkyl)imino, CH2, etc.; Z2 = CO, SO, P(O)(OH), etc.; p = 0 or 1] were prepared Thus, I (R = C6H4Br-3, R1R2 = CH:NCR8:CH, R8 = F) was condensed with 3-morpholinoprpanamine and the product acylated by CH2:CHCOCl to give title compound II. Data for biol. activity of I were given. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Reference of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

The Article related to quinazolinylacrylamide preparation tyrosine kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 26, 2017, Deng, Zeping; Chen, Fangjun published a patent.Computed Properties of 1187830-46-1 The title of the patent was Method for synthesizing pyrrolopyrimidine hydrochloride. And the patent contained the following:

The title method for synthesizing 6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride comprises reaction of furano[3,4-d]pyrimidine-5,7-dione, followed by reduction and salt formation. The experimental process involved the reaction of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride(cas: 1187830-46-1).Computed Properties of 1187830-46-1

The Article related to synthesis pyrrolopyrimidine hydrochloride imidation reduction, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 1187830-46-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On July 21, 2017, Liu, Shuangwei published a patent.Quality Control of 2-Methyl-7H-pyrrolo[2,3-d]pyrimidine The title of the patent was Process for preparation of pyrrolo[2,3-d]pyrimidine derivative for treating rheumatoid arthritis. And the patent contained the following:

The invention relates to preparation of pyrrolo[2,3-d]pyrimidine derivative of formula I, wherein R is Me, CF3, F, Ph for treating rheumatoid arthritis. Compound I was prepared via bromination of 2-Me-7-H-pyrrolo[2,3-d]pyrimidine followed by carboxylation, acylation, condensation and reaction with morpholine. The medicine has obvious therapeutic action to RA, and can be used for treating rheumatoid arthritis. The experimental process involved the reaction of 2-Methyl-7H-pyrrolo[2,3-d]pyrimidine(cas: 89792-07-4).Quality Control of 2-Methyl-7H-pyrrolo[2,3-d]pyrimidine

The Article related to pyrrolopyrimidine derivative preparation rheumatoid arthritis, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 2-Methyl-7H-pyrrolo[2,3-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On October 17, 2000, Pamukcu, Rifat; Piazza, Gary A. published a patent.Recommanded Product: 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine The title of the patent was Preparation of thienopyrimidines for inhibiting neoplastic cell growth. And the patent contained the following:

Title compounds [I; R = (un)substituted phenyl(alkyl); R1,R2 = H, halo, alkyl, alkoxy, etc.; R1R2 = alkylene; R3 = (un)substituted cycloalkyl, -heterocyclyl, -(hetero)aryl, etc.] were prepared for inhibiting neoplastic cell growth (no data). Thus, 2,4-dichloro-6-methylthieno[2,3-d]pyrimidine was aminated by 3,4-methylenedioxybenzylamine to give I (R = 3,4-methylenedioxybenzyl, R1 = Me, R2 = H)(II; R3 = Cl) which was condensed with Et piperidine-4-carboxylate to give II (R3 = 4-ethoxycarbonylpiperidino). The experimental process involved the reaction of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine(cas: 42518-42-3).Recommanded Product: 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine

The Article related to thienopyrimidine preparation neoplastic cell growth inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 17, 2016, Jonckers, Tim Hugo Maria; Mc Gowan, David Craig; Raboisson, Pierre Jean-Marie Bernard; Embrechts, Werner Constant Johan; Guillemont, Jerome Emile Georges published a patent.HPLC of Formula: 89792-07-4 The title of the patent was Preparation of pyrrolopyrimidines for the treatment of influenza virus infection. And the patent contained the following:

Title compounds I [X = N or C (optionally substituted with -CN, -CF3, -CONH2, etc.); R1 = H or CH3; R2 = H or NH2; R3 = carboxy-substituted alkyl, carboxy-substituted cycloalkyl, -N-alkylsulfone, etc.; or stereoisomeric forms, pharmaceutically acceptable salts, solvates, or polymorphs thereof] were prepared For example, reaction of 2,4-dichloro-5-fluoropyrimidine with cis-N-(3-aminocyclohexyl)pyrrolidine-1-carboxamide/DIPEA followed by Pd(PPh3)4-catalyzed coupling reaction with 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidine and deprotection using NaOMe afforded compound II. In anti-influenza activity test against A/Taiwan/1/86 (H1N1) virus, IC50 value of II was 0.005 μM. The experimental process involved the reaction of 2-Methyl-7H-pyrrolo[2,3-d]pyrimidine(cas: 89792-07-4).HPLC of Formula: 89792-07-4

The Article related to pyrrolopyrimidine preparation influenza virus infection treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 89792-07-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia