Category: pyrimidines

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

On October 16, 2002, Bhattacharya, Samit Kumar; Kath, John Charles; Morris, Joel published a patent.Category: pyrimidines The title of the patent was Preparation of substituted bicyclo[]-4-amino-pyridopyrimidine derivatives as kinase inhibitors. And the patent contained the following:

Title compounds I [R1-2 = H, alkyl; R3 = (CR1R2)mR4; m = 0-6 or NR1R3 = (CR1R2)n-indol(in)yl; n = 0-2; X = N and Y is CR9 or X = CR9 and Y = N; R9 = fused-ring bicyclic, bridged bicyclic or spirobicylic group] were prepared For instance, 4-chloro-6-fluoropyrido[3,4-d]pyrimidine (preparation given) was reacted with [3-methyl-4-(pyridin-3-yloxy)phenyl]amine (t-BuOH/ClCH2CH2Cl, reflux, 1 h) and the product coupled to (3-azabicyclo[3.1.0]hex-6-yl)carbamic acid tert-Bu ester (EtOH, sealed tube, 105°, 24 h) and finally deprotected to give II. Selected compounds of the invention had IC50 in the range of 1 nM to 1 pM for erbB-2 receptor kinase. I are used for the treatment of hyperproliferative disorders. 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 bicyclic amino pyridopyrimidine erbb2 kinase inhibitor preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: pyrimidines

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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

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 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 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 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

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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

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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 November 1, 2013, Lukmanov, Timur; Ivanov, Sergey P.; Khamitov, Edward M.; Khursan, Sergey L. published an article.SDS of cas: 626-48-2 The title of the article was Relative stability of keto-enol tautomers in 5,6-substituted uracils: Ab initio, DFT and PCM study. And the article contained the following:

The relative stability orders in the tautomers of uracil and its derivatives (5-fluorouracil, 5-chlorouracil, 5-aminouracil, 5-hydroxyuracil, 5-methyluracil, 6-methyluracil, 5-hydroxy-6-methyluracil and 5-amino-6-methyluracil) were established using composite (G3MP2B3) and DFT (TPSS) methods. The stability orders were determined both in the gas phase and water solutions, taking into account specific and non-specific hydration. The primary solvation shell of uracils was modeled as a complex of a tautomer with 5 water mols. An anal. of the factors which determine the stability of the enol forms of uracils was performed. The most important factor was found to be changes in the intramol. conjugation at tautomerization. As was shown by the NBO anal., the stabilization energy due to the nN → π* (or σ*) interaction in the diketo tautomer is lost in the enol forms, but is partially compensated by an increase in the conjugation length. The effect of the substituent in the fifth position of the pyrimidine ring on the energy of tautomers is less prominent. It was shown that the hydration energy considerably differs for tautomers, and leads to substantial redistribution in the stability series of uracil tautomers. Both specific and non-specific solvation are of vital importance for stabilization of tautomers. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).SDS of cas: 626-48-2

The Article related to uracil keto enol tautomer relative stability, Physical Organic Chemistry: Acid-Base, Tautomerism, and Other Equilibrium Studies and other aspects.SDS of cas: 626-48-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia