93129-68-1

Upstream product

• 63069-50-1 4-cyano-2-fluoroaniline 
• 108-24-7 acetic anhydride 
• 326-66-9 N-(4-bromo-2-fluorophenyl)acetamide 
• 557-21-1 dicyanozinc 
• 348-54-9 2-Fluoroaniline 
• 29632-74-4 2-fluro-4-iodoaniline 
• 97760-94-6 N-(2-fluoro-4-iodo-phenyl)-acetamide 
• 143-33-9 sodium cyanide 
• 35704-19-9 N-(4-cyanophenyl)acetamide 
• 544-92-3 copper(I) cyanide 

Downstream Products

• 849353-46-4 4-amino-3-fluoro-5-iodo-benzonitrile 
• 54240-29-8 1-(4-Amino-3-bromo-5-fluoro-phenyl)-2-(2-benzo[1,3]dioxol-5-yl-1-methyl-ethylamino)-ethanone 
• 54238-93-6 1-(4-Amino-3-chloro-5-fluoro-phenyl)-2-(2-benzo[1,3]dioxol-5-yl-1-methyl-ethylamino)-ethanone 
• 56340-31-9 4'-amino-3'-cyano-2-cyclopentylamino-5'-fluoroacetophenone 
• 56340-10-4 1-(4-Amino-3-bromo-5-fluoro-phenyl)-2-cycloheptylamino-ethanone 
• 56340-27-3 4'-amino-3'-cyano-2-cyclobutylamino-5'-fluoroacetophenone 
• 56340-25-1 4'-amino-3'-cyano-5'-fluoro-2-isopropylaminoacetophenone 
• 56340-23-9 4'-amino-3'-cyano-2-cyclopropylamino-5'-fluoroacetophenone 
• 771433-92-2 4'-acetylamino-3'-fluoro-2-isopropylamino-acetophenone 
• 56340-33-1 4'-amino-3'-cyano-5'-fluoro-2-tert-pentylaminoacetophenone 
• 685496-26-8 1-(4-Amino-3-chloro-5-fluoro-phenyl)-2-isopropylamino-ethanone 

Relevant academic research and scientific papers

NUCLIDE LABELLED H-TETRAZINES AND USE THEREOF FOR PET AND SPECT PRETARGETED IMAGING AND RADIONUCLIDE THERAPY

The present invention relates to novel tetrazine compounds for use in pretargeted in vivo imaging and in therapy and to the precursors of the tetrazine compounds. The compounds are suitable for use in click chemistry, i.e. reactions that join a targeting

NOVEL TETRAZINE COMPOUNDS FOR IN VIVO IMAGING

The present invention relates to novel tetrazine compounds of formula I, wherein one of R1-R5 is 18F, for use in pretargeted in vivo imaging. The compounds are suitable for use in click chemistry, i.e. reactions that join

1,1,1-TRIFLUORO-4-PHENYL-4-METHYL-2-(1H-PYRROLO

Compounds of Formula (IA), IB), IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: Structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents

Recently, 1,3-diarylalkyl thioureas have merged as one of the promising nonvanilloid TRPV1 antagonists possessing excellent therapeutic potential in pain regulation. In this paper, the full structure-activity relationship for TRPV1 antagonism of a novel series of 1,3-diarylalky thioureas is reported. Exploration of the structure-activity relationship, by systemically modulating three essential pharmacophoric regions, led to six examples of 1,3-dibenzyl thioureas, which exhibit Ca2+ uptake inhibition in rat DRG neuron with IC50 between 10 and 100 nM.

PHENYLALKYL AND PYRIDYLALKYL PIPERAZINE DERIVATIVES

This invention relates to compounds of the formula (1) wherein R1, R3, R4, X1, and X2 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.

COPPER-CATALYZED FORMATION OF CARBON-HETEROATOM AND CARBON-CARBON BONDS

One aspect of the present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-sulfur bond between the sulfur atom of a thiol moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper(II)-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-carbon bond between the carbon atom of cyanide ion and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In another embodiment, the present invention relates to a copper-catalyzed method of transforming and aryl, heteroaryl, or vinyl iodide. Yet another embodiment of the present invention relates to a tandem method, which may be practiced in a single reaction vessel, wherein the first step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl iodide from the corresponding aryl, heteroaryl, or vinyl chloride or bromide; and the second step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl nitrile, amide or sulfide from the aryl, heteroaryl, or vinyl iodide formed in the first step.

Copper-catalyzed domino halide exchange-cyanation of aryl bromides

An efficient copper-catalyzed domino halogen exchange-cyanation procedure for aryl bromides was developed utilizing 10 mol % CuI, 20 mol % KI, 1.0 equiv of the inexpensive N,N′-dimethylethylenediamine as ligand, and 1.2 equiv of NaCN in toluene at 110 °C. The new method represents a significant improvement over the traditional Rosenmund-von Braun reaction: the reaction conditions are much milder, and the use of stoichiometric amounts of copper(I) cyanide and polar solvents is avoided; therefore the isolation and purification of the aromatic nitrile products is greatly simplified. In addition, the new method exhibits excellent functional group compatibility comparable to that of the analogous Pd-catalyzed cyanation methodology. Copyright

Elemental fluorine Part 12. Fluorination of 1,4-disubstituted aromatic compounds

Direct fluorination of a series of 1,4-disubstituted benzene derivatives in acid reaction media at convenient temperature leads, in many cases, to selectively fluorinated aromatic products in preparatively useful conversions and yields.

Synthesis of further amino-halogen-substituted phenyl-aminoethanols

Starting from clenbuterol as a lead structure, new 4-amino-phenyl-aminoethanol analogues have been synthesized by different approaches. In these compounds one or both of the chlorine atoms of clenbuterol are replaced by other residues. This has led to compounds with high intrinsic β2-mimetic and/or β1-blocking activities. 1-(4-Amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert.-butylamino-ethanol hydrochloride (mabuterol) has been selected for clinical development. A detailed description is also given of the syntheses of new intermediate acetophenone derivatives as well as of the resolution of mabuterol into its enantiomers.