304693-64-9

Usage

Uses

Used in Pharmaceutical Industry:
Ethyl 2-(trifluoromethyl)pyrimidine-5-carboxylate is used as a key intermediate in the synthesis of NF-κB and AP-1 gene inhibitors. These inhibitors play a crucial role in regulating the expression of genes involved in inflammation, immune response, and cell proliferation. By targeting these transcription factors, Ethyl 2-(trifluoromethyl)pyrimidine-5-carboxylate contributes to the development of novel therapeutics for various diseases, including autoimmune disorders, chronic inflammation, and cancer.

InChI:InChI=1/C8H7F3N2O2/c1-2-15-6(14)5-3-12-7(13-4-5)8(9,10)11/h3-4H,2H2,1H3

Upstream product

• 92385-43-8 ethyl 3-(dimethylamino)-2-formylprop-2-enoate 
• 354-37-0 trifluoroacetamidine 
• 720-01-4 ethyl 2-trifluoromethyl-4-chloropyrimidine-5-carboxylate 
• 343-67-9 ethyl 2-(trifluoromethyl)-1,6-dihydro-6-oxopyrimidine-5-carboxylate 

Downstream Products

• 1192570-20-9 2-morpholin-4-yl-2-(2-trifluoromethyl-pyrimidin-5-yl)-ethylamine 
• 306960-78-1 2-trifluoromethylpyrimidine-5-carbonyl chloride 
• 306960-77-0 2-(trifluoromethyl)pyrimidine-5-carboxylic acid 

Relevant academic research and scientific papers

P2X3, RECEPTOR ANTAGONISTS FOR TREATMENT OF PAIN

The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor s

1,3-THIAZOL-2-YL SUBSTITUTED BENZAMIDES

The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.

Condensed pyrazole derivative

The present invention provides cyclic aminomethylpyrimidine derivatives and pharmaceutically acceptable salts thereof which show high selectivity for dopamine D4 receptors and are useful for treating diseases such as attention deficit hyperacti

NOVEL TRICYCLIC COMPOUNDS

The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.

P2X3, RECEPTOR ANTAGONISTS FOR TREATMENT OF PAIN

The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.

P2X3 RECEPTOR ANTAGONISTS FOR TREATMENT OF PAIN

The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X

Pyrimidinone compounds

Pyrimidinone compounds of formula (I) are inhibitors of the enzyme Lp-PLA2 and of use in therapy, in particular for treating atherosclerosis.

Potent, orally active inhibitors of lipoprotein-associated phospholipase A2: 1-(biphenylmethylamidoalkyl)-pyrimidones

A series of 1-(biphenylmethylamidoalkyl)-pyrimidones has been designed as nanomolar inhibitors of recombinant lipoprotein-associated phospholipase A2 with high potency in whole human plasma. 5-(Pyrazolylmethyl) derivative 16 and 5-(methoxypyrimidinylmethyl) derivative 27 demonstrated excellent pharmacodynamic profiles which correlated well with their pharmacokinetic effects.

Inhibitors of NF-kappaB and AP-1 gene expression: SAR studies on the pyrimidine portion of 2-chloro-4-trifluoromethylpyrimidine-5-[N-(3', 5'-bis(trifluoromethyl)phenyl)carboxamide].

We investigated the structure-activity relationship studies of N-[3, 5-bis(trifluoromethyl)phenyl][2-chloro-4-(trifluoromethyl)pyrimidin-5 -yl]carboxamide (1), an inhibitor of transcription mediated by both NF-kappaB and AP-1 transcription factors, with the goal of improving its potential oral bioavailability. Compounds were examined for cell-based activity, were fit to Lipinski's rule of 5, and were examined for potential gastrointestinal permeability using the intestinal epithelial cell line, Caco-2. Selected groups were substituted at the 2-, 4-, and 5-positions of the pyrimidine ring using solution-phase combinatorial methodology. The introduction of a fluorine in the place of 2-chlorine of 1 resulted in a compound with comparable activity. However, other substitutions at the 2-position resulted in a loss of activity. The trifluoromethyl group at the 4-position could be replaced with a methyl, ethyl, chlorine, or phenyl without a substantial loss of activity. The carboxamide group at the 5-position is critical for activity. If it was moved to the 6-position, the activity was lost. The 2-methyl analogue of 1 (81) showed comparable in vitro activity and improved Caco-2 permeability compared to 1.