89765-40-2

Upstream product

• 2338-76-3 3-trifluoromethylphenylacetonitrile 
• 74-88-4 methyl iodide 

Downstream Products

• 1179638-93-7 2-methyl-2-(3-(trifluoromethyl)phenyl)propan-1-amine 
• 1035261-95-0 diethyl 2-(2-methyl-2-(3-(trifluoromethyl)-phenyl)propanoyl)malonate 
• 82278-25-9 2-methyl-2-(3-(trifluoromethyl)phenyl)propanoic acid chloride 

Relevant academic research and scientific papers

Palladium-Catalyzed Distal m-C-H Functionalization of Arylacetic Acid Derivatives

Herein, we present m-C-H olefination on derivatives of phenylacetic acids by tethering with a simple nitrile-based template through palladium catalysis. Notably, the versatility of the method is evaluated with a wide range of phenylacetic acid derivatives for obtaining the meta-olefination products in fair to excellent yields with outstanding selectivities under mild conditions. Significantly, the present strategy is successfully exemplified for the synthesis of drugs/natural product analogues (naproxen, ibuprofen, paracetamol, and cholesterol).

Structure-activity relationship of N,N′-disubstituted pyrimidinetriones as CaV1.3 calcium channel-selective antagonists for Parkinson's disease

CaV1.3 L-type calcium channels (LTCCs) have been a potential target for Parkinson's disease since calcium ion influx through the channel was implicated in the generation of mitochondrial oxidative stress, causing cell death in the dopaminergic neurons. Selective inhibition of CaV1.3 over other LTCC isoforms, especially CaV1.2, is critical to minimize potential side effects. We recently identified pyrimidinetriones (PYTs) as a CaV1.3-selective scaffold; here we report the structure-activity relationship of PYTs with both CaV1.3 and CaV1.2 LTCCs. By variation of the substituents on the cyclopentyl and arylalkyl groups of PYT, SAR studies allowed characterization of the CaV1.3 and Ca V1.2 LTCCs binding sites. The SAR also identified four important moieties that either retain selectivity or enhance binding affinity. Our study represents a significant enhancement of the SAR of PYTs at CaV1.3 and CaV1.2 LTCCs and highlights several advances in the lead optimization and diversification of this family of compounds for drug development.

NAPHTHALENONE COMPOUNDS EXHIBITING PROLYL HYDROXYLASE INHIBITORY ACTIVITY, COMPOSITIONS, AND USES THEREOF

Compounds of Formula (I) and Formula (II) are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula(I) and Formula (II) have the following structures, where the definitions of the variables are provided herein.