29654-01-1

Upstream product

• 61272-76-2 4-fluoro-2-iodoaniline 
• 75-36-5 acetyl chloride 
• 351-83-7 4'-fluoroacetanilide 
• 371-40-4 4-fluoroaniline 
• 108-24-7 acetic anhydride 

Downstream Products

• 1184952-89-3 1-(3-(((4-(Dimethylamino)-4-phenylcyclohexyl)methoxy)methyl)-5-fluoro-2-(triethylsilyl)-1H-indol-1-yl)ethanone 
• 399-73-5 6-fluoro-2-methylbenzo[d]thiazole 
• 1620284-77-6 N-(4-fluoro-2-((trifluoromethyl)thio)phenyl)acetamide 
• 397-59-1 3-fluoro-10H-phenothiazine 
• 1352745-19-7 1-(5-fluoro-2,3-diphenyl-1H-indol-1-yl)ethan-1-one 

Relevant academic research and scientific papers

TRANSGLUTAMINASE 2 (TG2) INHIBITORS

Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit transglutaminase 2 (TG2). Also described herein are methods for using such TG2 inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from TG2 inhibition.

Cobalt(II)-catalyzed regioselective C-H halogenation of anilides

A cobalt-catalyzed regioselective C-H halogenation methodology is reported herein. The highlight of this work is the highly selective C-H functionalization of anilides, which results in high-yielding, versatile, and practical halogenated products. Thereby, brominations, chlorinations and iodinations of many electron-rich and electron-deficient anilides were achieved in a highly selective fashion. Mechanistic studies with respect to the pathway of the reaction are also described.

Synthesis and optical properties of 2-functionally substituted 4,5-dihydrothieno[3,2-c]quinolines

N-Protected 4-(anilinomethyl)thiophene-2-carbaldehydes were prepared by the reaction of easily available 4-chloromethylthiophene-2-carbaldehyde with N-(2-halogenophenyl) substituted acetamides, 4-methylbenzenesulfonamides and carbamates in the presence of K2CO3 or Cs2CO3. The compounds obtained were converted to 4,5-dihydrothieno [3,2-c]quinoline-2-carbaldehydes by palladium catalyzed intramolecular cyclization in homogenous or heterogenous (Pd/C) conditions with good yields and subsequently used for preparing of 2-functionally substituted thieno [3,2-c]quinoline derivatives (nitriles, carboxamides, carboxylic acids, esters). The optical properties of 2-functionally substituted thieno[3,2-c]quinolines and 4H-thieno[3,2-c]chromenes have been studied. Moderate to high fluorescence quantum yields are observed for these compounds ranging from 0.15 to 0.87. Structure - optical properties relationships have been established for the compounds synthesized, and their prospective application as invisible ink dyes was practically demonstrated.

Monoprotected l-Amino Acid (l-MPAA), Accelerated Bromination, Chlorination, and Iodination of C(sp2)?H Bonds by Iridium(III) Catalysis

Halogenated arenes are important structural motifs commonly found in biologically active molecules and used for a variety of transformations in organic synthesis. Herein, we report the mono-protected l-amino acid (l-MPAA) accelerated iridium(III)-catalyzed halogenation of (hetero)anilides at room temperature. This reaction constitutes the first example of an iridium(III)/l-MPAA-catalyzed general halogenation of (hetero)arenes through C(sp2)?H activation. Furthermore, we demonstrate the potential utility of our method through its use in the synthesis of a quinolone derivative.

Substituted 4-aminocyclohexane derivatives

Substituted 4-aminocyclohexane derivatives having the formula I: [image] wherein R1-R4 are as described herein, methods for their preparation, medicinal products and pharmaceutical compositions containing these compounds and the use of substituted 4-amino