281234-90-0

Upstream product

• 623-00-7 4-bromobenzenecarbonitrile 
• 35621-01-3 4-aminopiperidine dihydrochloride 
• 1452394-20-5 4-(4-azidopiperidin-1-yl)benzonitrile 
• 180695-80-1 tert-butyl 4-azidopiperidine-1-carboxylate 
• 73874-95-0 (piperidin-4-yl)carbamic acid tert-butyl ester 
• 1194-02-1 4-fluorobenzonitrile 
• 344566-78-5 tert-butyl (1-(4-cyanophenyl)piperidin-4-yl)carbamate 

Downstream Products

• 281234-89-7 4-(4-Amino-piperidin-1-yl)-benzoic acid 
• 1291057-90-3 4-[4-(3-benzo[b]thiophen-3-yl-3-hydroxypropylamino)piperidin-1-yl]benzonitrile 
• 1291057-83-4 4-[4-(3-benzo[b]thiophen-3-yl-3-oxopropylamino)piperidin-1-yl]benzonitrile 
• 247035-04-7 4-[4-{(tert-butoxycarbonyl)amino}piperidin-1-yl]benzoic acid 

Relevant academic research and scientific papers

Disubstituted 1-aryl-4-aminopiperidine library synthesis using computational drug design and high-throughput batch and flow technologies

A platform that incorporates computational library design, parallel solution-phase synthesis, continuous flow hydrogenation, and automated high throughput purification and reformatting technologies was applied to the production of a 120-member library of 1-aryl-4-aminopiperidine analogues for drug discovery screening. The application described herein demonstrates the advantages of computational library design coupled with a flexible, modular approach to library synthesis. The enabling technologies described can be readily adopted by the traditional medicinal chemist without extensive training and lengthy process development times.

Novel benzo[ b ]thiophene derivatives as new potential antidepressants with rapid onset of action

We report benzo[b]thiophene derivatives synthesized according to a dual strategy. 8j, 9c, and 9e with affinity values toward 5-HT7R and 5-HTT were selected to probe their antidepressant activity in vivo using the forced swimming text (FST). The results showed significant antidepressant activity after chronic treatment. 9c was effective in reducing the immobility time in FST even after acute treatment. These findings identify these compounds as a new class of antidepressants with a rapid onset of action.

Non-nucleoside reverse transcriptase inhibitors

The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5a, R5b, R6a, R6b and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.

SUBSTITUTED (AMINOIMINOMETHYL OR AMINOMETHYL) BENZOHETEROARYL COMPOUNDS

This invention is directed to an (aminoiminomethyl or aminomethyl) benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.

Remarkably selective palladium-catalyzed amination process: Rapid assembly of multiamino based structures

Palladium-catalyzed selective amination by a primary amine in the presence of a secondary amine provided up to >99:1 selectivity with high yields.