Tag: 200-300

On February 11, 2016, Claremon, David A.; Dong, Chengguo; Fan, Yi; Leftheris, Katerina; Lotesta, Stephen D.; Singh, Suresh B.; Tice, Colin M.; Zhao, Wei; Zheng, Yajun; Zhuang, Linghang published a patent.Quality Control of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine The title of the patent was Preparation of piperazine derivatives as liver X receptor modulators. And the patent contained the following:

Provided are novel compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are liver X receptor modulators, and which are useful in the treatment of diseases and disorders associated with the liver X receptor. Also provided are the compounds of formula I and pharmaceutical compositions thereof for treating atherosclerosis, cardiovascular disease, Alzheimer’s disease, dermatitis, dyslipidemia, cancer and other diseases or disorders. Title compounds I [Q = alkyl-OC(O), heteroaryl, aryl-alkyl-OC(O), etc.; R1 = alkyl, cycloalkyl, aryl-alkyl, etc.; R2 = H, halo, cyano, etc.; R3 = alkyl, halo-alkyl, cycloalkyl, etc.; R4 = H or alkyl], and their pharmaceutically acceptable salts, are prepared Thus, e.g., II was prepared by reaction of (R)-tert-Bu 2-isopropylpiperazine-1-carboxylate with [3-(methylsulfonyl)phenyl]boronic acid. Compounds of the invention were evaluated for their LXr α/β binding ad agonist activity, e.g., II showed Ki value of 1690 nM and 157 nM on LXRα and LXRβ, resp. The experimental process involved the reaction of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine(cas: 785777-98-2).Quality Control of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine

The Article related to piperazine derivative preparation liver receptor lxr modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Quality Control of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 26, 2018, Wang, Fang; Zhang, Zhaochao; Li, Chong; Zhang, Xiaoqing published a patent.Category: pyrimidines The title of the patent was Process for preparation of organic compound based on pyridine and quinoxaline. And the patent contained the following:

The invention relates to preparation of organic compound based on pyridine and quinoxaline and application to OLED device. Compound I was prepared via multi step synthesis with coupling reactions as key steps. The compound has low absorption and high refractive index in visible light field, and can effectively improve light extraction efficiency of the OLED device when applied to CPL layer of the OLED device. The compound has deep HOMO energy level and high electronic mobility, can be used as a hole blocking/electron transport layer material of the OLED device, and can effectively block the hole or energy from being transferred from a light-emitting layer to one side of an electronic layer, so as to improve compounding efficiency of the hole and electron in the light-emitting layer, and further improve light emission efficiency and prolong service life of the OLED device. The experimental process involved the reaction of 5-Bromo-2,4,6-trichloropyrimidine(cas: 63931-21-5).Category: pyrimidines

The Article related to quinoxaline pyridine based organ compound preparation oled, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 11, 2020, Xing, Qifeng; Feng, Peichuan; Chen, Yue; Hu, Lingfeng; Chen, Yili published a patent.HPLC of Formula: 160377-42-4 The title of the patent was Organic compounds and its applications. And the patent contained the following:

An organic compound having simple and easy implementation, readily available raw materials, suitable for mass production scale-up and used as light emitting layer in an OLED device is provided. The class of organic compounds is represented by the following structural formula I as an example. The application of organic compound used in organic electroluminescent device. The experimental process involved the reaction of 5-(4-Bromophenyl)pyrimidine(cas: 160377-42-4).HPLC of Formula: 160377-42-4

The Article related to organic compound application electroluminescent device, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Three Or More Hetero Atoms and other aspects.HPLC of Formula: 160377-42-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On July 21, 2017, Zhang, Zhaochao; Li, Chong; Tang, Dandan; Jin, Weixin; Wang, Miao published a patent.Electric Literature of 63931-21-5 The title of the patent was Organic compounds based on pyridine and benzimidazole use as OLED device. And the patent contained the following:

The present invention provides chem. structural formula I of the organic compound, in which X1-X6 independently represents N or C atom, the number of N atoms is 2; p is 0, 1, 2, 3 or 4; m or n independently represents 0, 1, 2 or 3, m+n+z=4, Ar1-3 independently represents C1-10 linear chain or branched chain alkyl, halogen atom, protinium, deuterium, triterium atom substituted or unsubstituted Ph, naphthyl, anthracyl or pyridyl; pyrimidyl, pyrazinyl, pyridazinyl, dibenzopyrane, 9,9-di-Me fluorene, N-Ph carbazole, quinolyl, isoquinolyl or naphthyridinyl, Ar1 also represents single bond etc. The compound of this invention has higher glass transition temperature and mol. heat endurance; and it has low absorptivity and high refractive index in visible light domain. After applied to the CPL layer of OLED device, title compound can effectively enhance the light extraction efficiency of OLED device. The compound of this invention also has deep HOMO energy level and high electron mobility, so it can be used as material of hole barrier/electron transport layer of OLED device, and can effectively stop the conveyance of hole or energy from luminescent layer to electronic shell side, so as to enhance the compounding efficiency of hole and electron in luminescent layer, and enhance the luminous efficiency and service life of OLED device. The experimental process involved the reaction of 5-Bromo-2,4,6-trichloropyrimidine(cas: 63931-21-5).Electric Literature of 63931-21-5

The Article related to pyridine benzimidazole oled, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Electric Literature of 63931-21-5

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 28, 1983, Baram, S. G.; Shkurko, O. P.; Mamaev, V. P. published an article.Recommanded Product: 85386-20-5 The title of the article was Determination of substituent constants of p-substituted 2- and 5-pyrimidine groups using carbon-13 NMR. And the article contained the following:

The 13C NMR chem. shifts of I and II (R = H, Cl, MeO, NH2, Me2N, CO2Et, cyano) were used to calculate the inductive and resonance substituent constants of these 5-substituted 2-pyrimidyl and 2-substituted 5-pyrimidyl groups. Equations were obtained for the calculation of substituent constants for any 5(or 2)-substituted 2(or 5)-pyrimidyl groups. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).Recommanded Product: 85386-20-5

The Article related to nmr carbon phenylpyrimidine lfer, pyrimidine phenyl nmr carbon, substituent constant monosubstituted pyrimidyl group, Physical Organic Chemistry: Resonance Spectra (Electron Spin, Nuclear Magnetic and Fourier Transform Nuclear Magnetic, Quadrupole, etc.) and other aspects.Recommanded Product: 85386-20-5

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 28, 2010, Bury, Michael Jonathan; Cheung, Mui; Eidam, Hilary Schenck; Fox, Ryan Michael; Goodman, Krista; Manas, Eric Steven published a patent.SDS of cas: 85386-20-5 The title of the patent was Preparation of diazabicycloheptyl amino acid derivatives as transient receptor potential channel TRPV4 antagonists. And the patent contained the following:

Title compounds I [R1′ = (R1)i; i = 0-3; R1 = alkyl, alkoxy, CF3, halo, OCF3, CN, etc.; R2 = alkyl, cycloalkylmethyl, benzyl; R3 = (un)substituted pyrrolyl, pyrazolyl, tetrazolyl, isoquinolinyl,pyrimidinyl, etc.; ; G = (S,S)- or (R,R)-2,5-diazabicycloheptyl; X = a bond, CH2; Y = NH, N-alkyl, S; R5 = H, alkyl; and their pharmaceutically acceptable salts], were prepared Thus, a 5-step synthesis using 1,1-dimethylethyl (1S,4S)-2,5-diazabicyclo[2.2.1]heptane-2-carboxylate, 3-methyl-N-[[(phenylmethyl)oxy]carbonyl]-L-valine, and 1H-indole-2-carboxylic acid gave II. Tested title compounds inhibited TRPV4 with IC50 in the range of 1 nM to 10 μM. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).SDS of cas: 85386-20-5

The Article related to diazabicycloheptylaminoacid preparation transient receptor potential channel trpv4 antagonist, overactive bladder pain cardiovascular disease arthritis treatment diazabicycloheptane preparation and other aspects.SDS of cas: 85386-20-5

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 21, 2021, Kanouni, Toufike; Arnold, Lee D.; Kaldor, Stephen W.; Murphy, Eric A.; Tyhonas, John published a patent.Reference of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine The title of the patent was Preparation of 4-(pyrrolidin-1-yl)quinazoline, 4-(pyrrolidin-1-yl)isoquinoline, and 1-(pyrrolidin-1-yl)phthalazine derivatives as inhibitors of cyclin-dependent kinases. And the patent contained the following:

The title compounds represented by formula I [ring A = (un)substituted heteroaryl selected from pyridine, pyrazine, pyrimidine, quinoline, isoquinoline, quinazoline, pyrazolopyridine, pyrazolopyrimidine, thienopyrimidine, thienopyridine, pyridopyridine, pyridopyrimidine, or triazene; W = selected from a group having the structure Q-Q13; t = 1 or 2; u = 0, 1, or 2; R1, R2, R3 = each independently H or each (un)substituted C1-4 alkyl, or heterocyclyl(alkyl); R4 = H or (un)substituted C1-4 alkyl, or optionally, if R3 = (un)substituted C1-4 and R4 = (un)substituted, then R3 and R4 together join to form a ring; R5, R6 = each independently H, cyano,NH2, halo, or each (un)substituted C1-4 alkyl, C1-4 alkoxy, or C1-4 aminoalkyl; X = N or CH; Y = N, or C-L1-R11; Z = N or C-L2-R7; L1, L2 = each independently a bond, O, or N(R8); R7 = cyano, halo, or each (un)substituted C1-4 alkyl, C3-7 carbocyclyl, carbocyclyl(alkyl), heterocyclyl, heterocyclyl(alkyl); R8, R9, R10 = each independently H or (un)substituted C1-4 alkyl; R11 = H, cyano, halo, NH2, or each (un)substituted C1-4 alkyl, C3-7 carbocyclyl, carbocyclyl(alkyl), heterocyclyl, or heterocyclyl(alkyl)] or pharmaceutically acceptable salts or solvates thereof are prepared The compounds I are inhibitors of cyclin-dependent kinases (CDKs) and are useful for the treatment of cancer, neoplastic disease, or hyperproliferative disorder in human or animal. Thus, tert-Bu (R)-[1-(7-acrylamidoquinazolin-4-yl)pyrrolidin-3-yl]carbamate was stirred with CF3CO2H in CH2Cl2 at room temperature for 3 h to give (R)-N-[4-(3-aminopyrrolidin-1-yl)quinazolin-7-yl]acrylamide trifluoroacetate which was heated with 2-chloro-5-(trifluoromethyl)pyrimidine in the presence of diisopropylethylamine in DMSO at 80° for 30 min under nitrogen and microwave irradiation to give (R)-N-[4-[3-[[5-(trifluoromethyl)pyrimidin-2-yl]amino]pyrrolidin-1-yl]quinazolin-7-yl]acrylamide (II). II showed IC50 of ≤0.10μM against human recombinant CDK12. The experimental process involved the reaction of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine(cas: 785777-98-2).Reference of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine

The Article related to pyrrolidinylquinazoline pyrrolidinylisoquinoline pyrrolidinylphthalazine preparation inhibitor cyclin dependent kinase, cancer neoplastic disease hyperproliferative disorder treatment and other aspects.Reference of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 28, 2010, Bury, Michael Jonathan; Cheung, Mui; Eidam, Hilary Schenck; Fox, Ryan Michael; Goodman, Krista; Manas, Eric Steven published a patent.SDS of cas: 85386-20-5 The title of the patent was Preparation of diazabicycloheptyl amino acid derivatives as transient receptor potential channel TRPV4 antagonists. And the patent contained the following:

Title compounds I [R1′ = (R1)i; i = 0-3; R1 = alkyl, alkoxy, CF3, halo, OCF3, CN, etc.; R2 = alkyl, cycloalkylmethyl, benzyl; R3 = (un)substituted pyrrolyl, pyrazolyl, tetrazolyl, isoquinolinyl,pyrimidinyl, etc.; ; G = (S,S)- or (R,R)-2,5-diazabicycloheptyl; X = a bond, CH2; Y = NH, N-alkyl, S; R5 = H, alkyl; and their pharmaceutically acceptable salts], were prepared Thus, a 5-step synthesis using 1,1-dimethylethyl (1S,4S)-2,5-diazabicyclo[2.2.1]heptane-2-carboxylate, 3-methyl-N-[[(phenylmethyl)oxy]carbonyl]-L-valine, and 1H-indole-2-carboxylic acid gave II. Tested title compounds inhibited TRPV4 with IC50 in the range of 1 nM to 10 μM. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).SDS of cas: 85386-20-5

The Article related to diazabicycloheptylaminoacid preparation transient receptor potential channel trpv4 antagonist, overactive bladder pain cardiovascular disease arthritis treatment diazabicycloheptane preparation and other aspects.SDS of cas: 85386-20-5

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 21, 2021, Kanouni, Toufike; Arnold, Lee D.; Kaldor, Stephen W.; Murphy, Eric A.; Tyhonas, John published a patent.Reference of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine The title of the patent was Preparation of 4-(pyrrolidin-1-yl)quinazoline, 4-(pyrrolidin-1-yl)isoquinoline, and 1-(pyrrolidin-1-yl)phthalazine derivatives as inhibitors of cyclin-dependent kinases. And the patent contained the following:

The title compounds represented by formula I [ring A = (un)substituted heteroaryl selected from pyridine, pyrazine, pyrimidine, quinoline, isoquinoline, quinazoline, pyrazolopyridine, pyrazolopyrimidine, thienopyrimidine, thienopyridine, pyridopyridine, pyridopyrimidine, or triazene; W = selected from a group having the structure Q-Q13; t = 1 or 2; u = 0, 1, or 2; R1, R2, R3 = each independently H or each (un)substituted C1-4 alkyl, or heterocyclyl(alkyl); R4 = H or (un)substituted C1-4 alkyl, or optionally, if R3 = (un)substituted C1-4 and R4 = (un)substituted, then R3 and R4 together join to form a ring; R5, R6 = each independently H, cyano,NH2, halo, or each (un)substituted C1-4 alkyl, C1-4 alkoxy, or C1-4 aminoalkyl; X = N or CH; Y = N, or C-L1-R11; Z = N or C-L2-R7; L1, L2 = each independently a bond, O, or N(R8); R7 = cyano, halo, or each (un)substituted C1-4 alkyl, C3-7 carbocyclyl, carbocyclyl(alkyl), heterocyclyl, heterocyclyl(alkyl); R8, R9, R10 = each independently H or (un)substituted C1-4 alkyl; R11 = H, cyano, halo, NH2, or each (un)substituted C1-4 alkyl, C3-7 carbocyclyl, carbocyclyl(alkyl), heterocyclyl, or heterocyclyl(alkyl)] or pharmaceutically acceptable salts or solvates thereof are prepared The compounds I are inhibitors of cyclin-dependent kinases (CDKs) and are useful for the treatment of cancer, neoplastic disease, or hyperproliferative disorder in human or animal. Thus, tert-Bu (R)-[1-(7-acrylamidoquinazolin-4-yl)pyrrolidin-3-yl]carbamate was stirred with CF3CO2H in CH2Cl2 at room temperature for 3 h to give (R)-N-[4-(3-aminopyrrolidin-1-yl)quinazolin-7-yl]acrylamide trifluoroacetate which was heated with 2-chloro-5-(trifluoromethyl)pyrimidine in the presence of diisopropylethylamine in DMSO at 80° for 30 min under nitrogen and microwave irradiation to give (R)-N-[4-[3-[[5-(trifluoromethyl)pyrimidin-2-yl]amino]pyrrolidin-1-yl]quinazolin-7-yl]acrylamide (II). II showed IC50 of ≤0.10μM against human recombinant CDK12. The experimental process involved the reaction of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine(cas: 785777-98-2).Reference of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine

The Article related to pyrrolidinylquinazoline pyrrolidinylisoquinoline pyrrolidinylphthalazine preparation inhibitor cyclin dependent kinase, cancer neoplastic disease hyperproliferative disorder treatment and other aspects.Reference of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On June 1, 2012, Li, Zhenhua; Wu, Danli; Zhong, Weihui published an article.Safety of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine The title of the article was Facile and efficient cyclization of anthranilonitrile to 2,4-dichloroquinazoline by bis(trichloromethyl) carbonate and catalytic amount triphenylphosphine oxide. And the article contained the following:

2,4-Dichloroquinazolines were synthesized by the cyclization of anthranilonitrile using bis(trichloromethyl)carbonate with the aid of catalytic amount of Ph3PO at 120 °C. This method was also applied to the synthesis of 2,4-dichlorothieno[2,3-d]pyrimidine. The plausible mechanism was presented. The experimental process involved the reaction of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine(cas: 42518-42-3).Safety of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine

The Article related to anthranilonitrile chloromethylcarbonate cyclization phenylphosphine oxide catalyst, aminothiophenonitrile chloromethylcarbonate cyclization phenylphosphine oxide catalyst, chloroquinazoline preparation, chlorothienopyrimidine preparation and other aspects.Safety of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia