113259-79-3

Upstream product

• 6628-86-0 5-chloro-2-nitrobenzaldehyde 
• 110-89-4 piperidine 
• 20357-20-4 5-bromo-2-nitrobenzaldehyde 
• 26908-35-0 5-chloro-2-nitrobenzaldehyde ethylene acetal 
• 113260-03-0 5-(piperidin-1-yl)-2-nitrobenzaldehyde ethylene acetal 
• 2516-95-2 5-chloro-2-nitrobenzoic acid 
• 73033-58-6 5-chloro-2-nitrobenzyl alcohol 

Downstream Products

• 113259-86-2 5-<<2-nitro-5-(1-piperidinyl)phenyl>methylene>-2,4-imidazolidinedione 
• 118159-40-3 5-(piperidin-1-yl)-2-nitrobenzyl alcohol 
• 1354826-24-6 (2-nitro-5-(piperidin-1-yl)phenyl)(1-(phenylsulfonyl)-6-(trifluoromethyl)-1H-indol-2-yl)methanone 
• 1354826-25-7 (2-amino-5-(piperidin-1-yl)phenyl)-(1-(phenylsulfonyl)-6-(trifluoromethyl)-1H-indol-2-yl)methanone 
• 1354826-26-8 methyl 3-(3-((2-(1-(phenylsulfonyl)-6-(trifluoromethyl)-1H-indole-2-carbonyl)-4-(piperidin-1-yl)phenyl)carbamoyl)benzylthio)propanoate 
• 1354826-28-0 methyl 3-(3-((4-(piperidin-1-yl)-2-(6-(trifluoromethyl)-1H-indole-2-carbonyl)phenyl)carbamoyl)benzylthio)propanoate 
• 1354826-19-9 3-(3-((4-(piperidin-1-yl)-2-(6-(trifluoromethyl)-1H-indole-2-carbonyl)phenyl)-carbamoyl)-benzylthio)-propanoic acid 
• 1354826-31-5 N₁-methyl-N₁-(2-morpholinoethyl)-N₃-(2-(1-(phenylsulfonyl)-6-(trifluoromethyl)-1H-indole-2-carbonyl)-4-(piperidin-1-yl)phenyl)isophthalamide 
• 1354826-21-3 N₁-methyl-N₁-(2-morpholinoethyl)-N₃-(4-(piperidin-1-yl)-2-(6-(trifluoromethyl)-1H-indole-2-carbonyl)phenyl)isophthalamide 2,2,2-trifluoroacetate 
• 1354826-23-5 (2-nitro-5-(piperidin-1-yl)phenyl)(1-(phenylsulfonyl)-6-(trifluoromethyl)-1H-indol-2-yl)methanol 

Relevant academic research and scientific papers

Protecting-group-free amination of halogenated nitrobenzaldehyde with palladium catalyst

"One-step" method for the synthesis of secondary aliphatic amine substituted nitrobenzaldehyde was developed. In the presence of Pd catalyst, halogenated nitrobenzaldehyde could be smoothly coupled with secondary aliphatic amine to give the target product

COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT

Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically ac

New safety-catch photolabile protecting group

Photolabile protecting groups have proven their usefulness on many occasions. Their versions as linkers are however less attractive, as robustness and real orthogonality become critical issues. Safety-catch systems, where a preliminary activation phase is necessary, circumvent the problem of premature cleavage. In this work, we introduce a new safety-catch photolabile protecting group, whose cleavage requires the simultaneous presence of light and a chemical promoter.

Inhibitors of Blood Platelet cAMP Phosphodiesterase. 3. 1,3-Dihydro-2H-imidazoquinolin-2-one Derivatives with Enhanced Aqueous Solubility

Two series of 1,3-dihydro-2H-imidazoquinolin-2-one derivatives incorporating an additional site for acid salt formation were synthesized and evaluated as inhibitors of human blood platelet cAMP phosphodiesterase (PDE) and ADP-induced platelet aggregation.The objective of this study was to identify compounds that blended potent biological activity with a satisfactory level of aqueous solubility.From a series of 7-aminoimidazoquinolin-2-ones, biological and physical properties were optimally combined in the 1-piperidinyl derivative 11c.However, this compound offered no significant advantage over earlier studied compounds as an antithrombotic agent in an animal model of small vessel thrombosis.A series of 7-alkoxy alkanoic piperazinamide derivatives, in which the additional basic nitrogen atom was remote from the heterocyclic nucleus and accomodated in a secondary binding region of the cAMP PDE enzyme, demonstrated greater intrinsic cAMP PDE inhibitory activity.Structural modifications of this series focused on variation of the piperazine substituent and side-chain length.The lipophilicity of the N-substituent influenced biological potency and aqueous solubility, with substituents of seven carbon atoms or less generally providing acceptable solubility properties.The N-(cyclohexylmethyl)piperazinamide 21h was identified from this series of compounds as a potent inhibitor of platelet cAMP PDE, IC50 = 0.4 nM and ADP-induced platelet aggregation, IC50 = 0.51 μM after a 3-min exposure and 0.1 μM after a 15-min exposure of platelet-rich plasma to the drug.Evaluation of 21h and representative analogues in vivo using a rabbit model of small vessel thrombosis revealed significantly greater antithrombotic efficacy compared to that of previously studied compounds with similar intrinsic biological activity measured in vitro but inferior aqueous solubility.

7-amino-1,3-dihydro-2H-imidazo[4,5-b]quinolin 2-ones and method for inhibiting phosphodiesterase and blood platelet aggregation

Novel series of 2,3-dihydro-2-oxo-1H-imidazo[4,5-b]quinolinyl amine derivatives of Formula STR1 wherein R1 is hydrogen, lower alkyl; R2 is hydrogen, lower alkyl, lower alkoxy, halogen; R3 is hydrogen, lower alkyl; R4 is hydrogen, lower alkyl, alkanoyl, phenylalkanoyl wherein phenyl is optionally substituted with halogen, lower alkyl, lower alkoxy; R3 and R4 are joined together to form morpholinyl, piperidinyl or pyrrolidinyl optionally substituted with --CO2 R5 or STR2 wherein R5 is hydrogen or lower alkyl, and R6 is hydrogen, lower alkyl, cycloalkyl; 4-R7 -piperazinyl wherein R7 is --CO2 R8 wherein R8 is lower alkyl, phenyl optionally substituted with up to 2 halogen, lower alkyl or lower alkoxy; phenylalkanoyl of 7 to 10 carbon wherein phenyl is unsubstituted or independently substituted with up to 2 halogen, lower alkyl, lower alkoxy. The compounds are cyclic AMP phosphodiesterase inhibitors and are particularly useful as inhibitors of blood platelet aggregation and/or as cardiotonic agents.