Category: 785777-98-2

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 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 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