159182-10-2

Upstream product

• 13472-00-9 p-Aminophenethylamine 
• 501-53-1 benzyl chloroformate 
• 3544-25-0 p-aminophenylacetonitrile 
• 29968-78-3 2-(4-nitrophenyl)ethylamine monohydrochloride 
• 13139-17-8 N-(Benzyloxycarbonyloxy)succinimide 
• 182252-00-2 N-benzyloxycarbonyl-4-nitrophenethylamine 

Downstream Products

• 909534-41-4 benzyl 4-(2,6-dimethyl-3-nitropyridin-4-ylamino)phenethylcarbamate hydrochloride 
• 159182-19-1 N-[4-[2-[(phenylmethoxycarbonyl)amino]ethyl]phenyl]-2-naphthalenesulfonamide 

Relevant academic research and scientific papers

triAZOLOtriAZINE DERIVATIVES AS A2A RECEPTOR ANTAGONISTS

The present invention provides triazolotriazine derivatives of formula (1) as A2A receptor antagonists. Compounds of formula (1) and pharmaceutical compositions including the compounds can be used for the treatment of disorders related to A2A receptor hyperfunctioning, such as certain types cancers. Compounds of formula (1) and methods of preparing the compounds are disclosed in the invention.

Microwave-assisted protection of primary amines as 2,5-dimethylpyrroles and their orthogonal deprotection

Primary amines can be readily doubly protected as N-substituted 2,5-dimethylpyrroles. Although this protecting group is stable toward strong bases and nucleophiles, long reaction times are required for both the protection and deprotection steps, generally resulting in low deprotection yields. By employing microwave irradiation, protection and deprotection reaction times are dramatically reduced. Furthermore, deprotection with dilute hydrochloric acid in ethanol increases reaction yields. Diverse deprotection conditions have been developed in conjunction with microwave irradiation, so that protection as an N-substituted 2,5-dimethylpyrrole can be orthogonal to other standard amine protecting groups, such as tert-butyloxycarbonyl (Boc), carbobenzyloxy (Cbz), and 9-fluorenylmethyloxycarbonyl (Fmoc).

INHIBITION OF BACTERIAL BIOFILMS WITH ARYL CARBAMATES

Disclosure is provided for carbamate compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.

USE OF ARYL CARBAMATES IN AGRICULTURE AND OTHER PLANT-RELATED AREAS

Disclosure is provided for methods of preventing, removing or inhibiting microbial biofilm formation or microbial infection in a plant or plant part thereof, including applying thereto a treatment effective amount of an aryl carbamate as described herein,

Synthesis and application of a triazene?ferrocene modifier for immobilization and characterization of oligonucleotides at electrodes

A new DNA modifier containing triazene, ferrocene, and activated ester functionalities was synthesized and applied for electrochemical grafting and characterization of DNA at glassy carbon (GC) and gold electrodes. The modifier was synthesized from ferrocenecarboxylic acid by attaching a phenyltriazene derivative to one of the ferrocene Cp rings, while the other Cp ring containing the carboxylic acid was converted to an activated ester. The modifier was conjugated to an amine-modified DNA sequence. For immobilization of the conjugate at Au or GC electrodes, the triazene was activated by dimethyl sulfate for release of the diazonium salt. The salt was reductively converted to the aryl radical which was readily immobilized at the surface. DNA grafted onto electrodes exhibited remarkable hybridization properties, as detected through a reversible shift in the redox potential of the Fc redox label upon repeated hybridization/denaturation procedures with a complementary target DNA sequence. By using a methylene blue (MB) labeled target DNA sequence the hybridization could also be followed through the MB redox potential. Electrochemical studies demonstrated that grafting through the triazene modifier can successfully compete with existing protocols for DNA immobilization through the commonly used alkanethiol linkers and diazonium salts. Furthermore, the triazene modifier provides a practical one-step immobilization procedure.

Synthesis and bacterial biofilm inhibition studies of ethyl N-(2-phenethyl) carbamate derivatives

An 88 member library based upon the marine bacterial metabolite ethyl N-(2-phenethyl) carbamate was evaluated for bacterial biofilm inhibition against a panel of medically relevant strains. These studies culminated in the discovery of a new class of molec

CRYSTAL FORMS OF AN IMIDAZOLE DERIVATIVE

The invention relates to the essentially pure Λ/-[({2-[4-(2-Ethyl-4,6-dimethyl-1 H- imidazo[4,5-c]pyridin-1 -yl)phenyl]ethyl}amino)carbonyl]-4- methylbenzenesulfonamide Polymorph Forms A and B and to processes for the preparation of, compositions containi

Pd/C(en)-catalyzed chemoselective hydrogenation with retention of the N-Cbz protective group and its scope and limitations

A chemoselective method for the hydrogenation of acetylene, olefin, azide, nitro and benzyl ester functionalities with retention of the aliphatic N-Cbz group was established. The chemoselectivity was accomplished by using a combination of 5% Pd/C-ethylenediamine [5% Pd/C(en)] and THF (or 1,4-dioxane) as a solvent, and the scope and limitations of this methodology were investigated. These results reinforce the utility of N-Cbz protective groups in synthetic chemistry, especially in peptide synthesis. (C) 2000 Elsevier Science Ltd.

Substituted phenyl sulfonamides as selective β 3 agonists for the treatment of diabetes and obesity

Substituted phenylsulfonamides are selective β 3 adrenergic receptor agonists with very little β 1 and β 2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted alkyl epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.