86847-83-8

Upstream product

• 1072-98-6 5-chloro-2-pyridylamine 
• 3282-30-2 pivaloyl chloride 
• 121953-45-5 (1-Benzotriazol-1-yl-2,2-dimethyl-propyl)-(5-chloro-pyridin-2-yl)-amine 
• 86847-59-8 2-(pivaloylamino)pyridine 

Downstream Products

• 705291-49-2 2-(tert-butylcarbonylamino)-5-chloronicotinic acid 
• 35170-93-5 3-chloro-1,8-naphthyridine 

Relevant academic research and scientific papers

Chlorination Reaction of Aromatic Compounds and Unsaturated Carbon-Carbon Bonds with Chlorine on Demand

Chlorination with chlorine is straightforward, highly reactive, and versatile, but it has significant limitations. In this Letter, we introduce a protocol that could combine the efficiency of electrochemical transformation and the high reactivity of chlorine. By utilizing Cl3CCN as the chloride source, donating up to all three chloride atom, the reaction could generate and consume the chlorine in situ on demand to achieve the chlorination of aromatic compounds and electrodeficient alkenes.

Optimization of 5-substituted thiazolyl ureas and 6-substituted imidazopyridines as potential HIV-1 latency reversing agents

A persistent latent reservoir of virus in CD4+ T cells is a major barrier to cure HIV. Activating viral transcription in latently infected cells using small molecules is one strategy being explored to eliminate latency. We previously described the use of a FlpIn.FM HEK293 cellular assay to identify and then optimize the 2-acylaminothiazole class to exhibit modest activation of HIV gene expression. Here, we implement two strategies to further improve the activation of viral gene expression and physicochemical properties of this class. Firstly, we explored rigidification of the central oxy-carbon linker with a variety of saturated heterocycles, and secondly, investigated bioisosteric replacement of the 2-acylaminothiazole moiety. The optimization process afforded lead compounds (74 and 91) from the 2-piperazinyl thiazolyl urea and the imidazopyridine class. The lead compounds from each class demonstrate potent activation of HIV gene expression in the FlpIn.FM HEK293 cellular assay (both with LTR EC50s of 80 nM) and in the Jurkat Latency 10.6 cell model (LTR EC50 220 and 320 nM respectively), but consequently activate gene expression non-specifically in the FlpIn.FM HEK293 cellular assay (CMV EC50 70 and 270 nM respectively) manifesting in cellular cytotoxicity. The lead compounds have potential for further development as novel latency reversing agents.

METHODS AND COMPOSITIONS FOR INHIBITION OF BROMODOMAIN-CONTAINING PROTEINS

The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.

Rhodium(III)-catalyzed oxidative olefination of pyridines and quinolines: Multigram-scale synthesis of naphthyridinones

A Rh(III)-catalyzed oxidative olefination of pyridines and quinolines has been achieved. This method has a broad substrate scope and has been applied to the expeditious, multigram-scale synthesis of naphthyridinones.

5, 7-DIHYDRO- 6H-PYRIMIDO [ 5, 4-D] [ 1 ] BENZAZEPIN-6-THIONES AS PLK INHIBITORS

This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors

A series of 3,4,6-substituted 2-quinolones has been synthesized and evaluated as inhibitors of the kinase domain of macrophage colony-stimulating factor-1 receptor (FMS). The fully optimized compound, 4-(4-ethyl-phenyl)-3-(2-methyl-3H-imidazol-4-yl)-2-qui

CCR9 INHIBITORS AND METHODS OF USE THEREOF

The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.

Substituted benzopyran analogs for the treatment of inflammation

A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I'wherein X, A1, A2, A3, A4, R, R'', R1 and R2 are as described in the specification.

Substituted benzopyran derivatives for the treatment of inflammation

A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I'wherein X, A1, A2, A3, A4, R, R'', R1 and R2 are as described in the specification.

The Chemistry of N-Substituted Benzotriazoles. Part 20. Mono-N-t-Butylation of Aromatic and Heteroaromatic Amines

Adducts R1CH(Bt)NHAr, readily available from aldehydes, primary aromatic or heteroaromatic amines, and benzotriazole are converted by H2O2-SeO2 into mixtures of R1CONHAr and HCONR1Ar in proportions which depend rationally on the nature of the R1 group.For R1=But, the formamide HCON(But)Ar is formed in satisfactory yields thus enabling the title reaction to be achieved.