20974-36-1

Upstream product

• 22745-75-1 4-(3-cyano-3,3-diphenyl-propyl)-piperazine-1-carboxylic acid ethyl ester 
• 143816-97-1 4-(3,3-Diphenyl-propyl)-piperazine-1-carboxylic acid ethyl ester 
• 18903-01-0 trans-1-cinnamylpiperazine 
• 71-43-2 benzene 
• 606-83-7 3,3-Diphenylpropionic acid 
• 37089-77-3 3,3-diphenylpropanoyl chloride 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 41140-53-8 1-Methanesulfonyloxy-3,3-diphenylpropane 
• 110-85-0 piperazine 
• 20017-68-9 1-bromo-3,3-diphenylpropane 
• 1391748-29-0 C₂₄H₃₂N₂O₂ 
• 348611-34-7 4-(3,3-Diphenyl-propionyl)-piperazine-1-carboxylic acid ethyl ester 
• 23808-47-1 3,3-diphenylpropyl 4-methylbenzenesulfonate 
• 23426-03-1 3,3-diphenylpropanoic acid methyl ester 

Downstream Products

• 137075-07-1 1-(3,3-diphenylpropyl)-4-(pyridin-3-ylcyanomethyl)piperazine 
• 301666-12-6 ethyl 2-cyano-5-[4-(3,3-diphenyl-1-propyl)piperazin-1-yl]benzoate 
• 137074-07-8 1-(2-Naphthoyl)-4-(3-pyridylcyanomethyl)piperazine, dihydrochloride 
• 1092850-44-6 10-[4-(4-(3,3-diphenylpropyl)piperazino)butyl]phenothiazine 

Relevant academic research and scientific papers

Hydrogenated acridine derivative and its application

The invention relates to the field of chemical synthesis, and particularly relates to a compound with the general formula being Y-L-X and an application of the compound serving as a calcium channel blocking agent or/and an acetylcholinesterase inhibitor. The compound with the general formula being Y-L-X can be used for adjusting calcium homeostasis and treating cardiovascular diseases, stroke or dementia.

Synthesis and evaluation of 4-substituted piperidines and piperazines as balanced affinity μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands

In this letter, we describe a series of 4-substituted piperidine and piperazine compounds based on tetrahydroquinoline 1, a compound that shows balanced, low nanomolar binding affinity for the mu opioid receptor (MOR) and the delta opioid receptor (DOR).

New 1,3-dioxolane and 1,3-dioxane derivatives as effective modulators to overcome multidrug resistance

Multidrug resistance (MDR) to antitumor agents represents a major obstacle to a successful chemotherapy of cancer. Overexpression of P-glycoprotein (p-gp) seems to be the major factor responsible for MDR. A large number of chemically unrelated compounds are known to interact with p-gp resulting in a decreasing resistance. In our efforts related to structure-activity studies of new potential MDR reversal agents we synthesized a series of compounds that differ in the aromatic core structure, the linker, and the basic moiety. For our search of new aromatic core structures we synthesized novel 2,2-diphenyl-1,3-dioxolane, 2,2- diphenyl-1,3-dioxane, and 4,5-diphenyl-1,3-dioxolane derivatives. A range of lipophilic linker structures and protonable basic moieties were synthesized and investigated to optimize the structure of the potential MDR-modulators. The compounds were tested in vitro using human Caco-2 cells. Both the cytotoxicity of the synthons and their ability to resensitize the cells were determined with a MTT assay. The results show that at low concentration various substances reverse tumor cell MDR. Some of the new structures show better effects than established modulators like trifluoperazine.

Dicationic electrophiles from olefinic amines in superacid

This paper describes the superacid-catalyzed chemistry of olefinic amines and related compounds. A variety of olefinic amines are found to react with benzene in CF3SO3H (triflic acid) to give addition products in good yields (75-99%), including the pharmaceutical agents fenpiprane and prozapine. A general mechanism is proposed that invokes the formation of reactive, dicationic electrophiles and the direct observation of a diprotonated species is reported from low-temperature NMR experiments. This chemistry is also used to conveniently prepare functionalized polystyrene beads having pendant amine groups.

DIARYLALKYL CYCLIC DIAMINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS

Cyclic diamines of formula (I) or their pharmacologically acceptable acid addition salts, and their medical applications are described. These compounds inhibit the action of chemokines such as MIP-la and/or MCP-l on target cells, and are useful as a therapeutic drug and/or preventative drug in diseases, such as atherosclerosis, rheumatoid arthritis, and the like where blood monocytes and lymphocytes infiltrate into tissues.

(Pyridylcyanomethyl)piperazines as orally active PAF antagonists

A series of (pyridylcyanomethyl)piperazines was prepared and evaluated for PAF-antagonist activity. Compounds were tested in vitro in a PAF-induced platelet aggregation assay and in vivo in a PAF-induced hypotension test in normotensive rats. Oral activity was ascertained through a PAF-induced mortality test in mice. The main structure-activity trends of the series were established. Activity was mainly found in four skeletons: 1-acyl-4-(3- pyridylcyanomethyl)-piperazine, 1-acyl-4-(4-pyridylcyanomethyl)piperazine, 1- acyl-4-(3-pyridylcyanomethyl)piperidine, and 1-acyl-4-cyano-4-(3- pyridylamino)piperidine. The acyl substituents, diphenylacetyl and 3,3- diphenylpropionyl, provided the most active compounds, and the introduction of an amine or hydroxy group in the 3,3-diphenylpropionyl substituent led to further improvement in oral activity. As a result, three of the most active compounds (100, 114, and 115) have been selected for further pharmacological development.