33259-72-2

Usage

Uses

Used in Pharmaceutical Industry:
5,6-DIAMINO-2-PICOLINE is used as a key intermediate in the synthesis of pharmaceuticals for its ability to contribute to the development of new drugs and medicinal compounds. Its unique chemical structure allows for the creation of molecules with specific therapeutic properties, enhancing the range of treatments available for various health conditions.
Used in Agrochemical Industry:
In the agrochemical sector, 5,6-DIAMINO-2-PICOLINE serves as an essential intermediate in the production of agrochemicals, such as pesticides and herbicides. Its involvement in the synthesis of these compounds helps to improve crop protection and yield, contributing to more efficient and sustainable agricultural practices.
Used in Organic Synthesis:
5,6-DIAMINO-2-PICOLINE is utilized in organic synthesis for its versatility in forming various chemical bonds and structures. This property makes it a valuable component in the creation of a wide range of organic compounds, which can be applied across different industries, including chemical manufacturing, materials science, and research.
Used in Research and Development:
As a chemical intermediate, 5,6-DIAMINO-2-PICOLINE is also employed in research and development settings. Scientists and researchers use 5,6-DIAMINO-2-PICOLINE, to explore new chemical reactions, investigate its potential applications, and develop innovative products and processes that can benefit various industries.
It is important to handle and store 5,6-DIAMINO-2-PICOLINE with caution, as it can be harmful if ingested, inhaled, or comes into contact with skin. Proper safety measures should be taken to ensure the well-being of individuals working with 5,6-DIAMINO-2-PICOLINE,.

InChI:InChI=1/C6H9N3/c1-4-2-3-5(7)6(8)9-4/h2-3H,7H2,1H3,(H2,8,9)/p+1

Upstream product

• 19346-45-3 2-fluoro-3-nitro-6-methylpyridine 
• 39745-40-9 2-chloro-6-methyl-3-aminopyridine 
• 21901-29-1 6-amino-5-nitro-2-picoline 
• 1824-81-3 2-Amino-6-methylpyridine 

Downstream Products

• 27582-24-7 5-methylpyridol[2,3-d]imidazole 
• 59352-86-2 6-methyl-2,3-diphenyl-pyrido[2,3-b]pyrazine 
• 220658-95-7 2-aminomethyl-5-methyl-1(H)-imidazo-4-pyridine 
• 193534-43-9 {4-methyl-7-[(5-methyl-1H-imidazo[4,5-b]pyridin-2-ylmethyl)-carbamoyl]-3-oxo-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepin-2-yl}-acetic acid methyl ester 
• 133241-05-1 5-Methyl-2-propyl-3-[2'-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazo[4,5-b]pyridine 
• 577777-16-3 (5-methyl-1H-imidazo[4,5-b]pyridin-2-yl)acetonitrile 
• 954218-99-6 C₈H₉N₃O 
• 175530-95-7 2-[[N-(Benzyloxycarbonyl)-N-methyl]aminomethyl]-5-methyl4-azabenzimidazole 
• 159104-35-5 (3RS)-3,6-Dimethyl-3,4-dihydro-1,4,5-triazanaphthalen-2(1H)-one 
• 116035-71-3 2-chloro-5-methyl-1H-imidazo[4,5-b]pyridine 
• 193533-15-2 (5-methyl-1H-imidazo[4,5-b]pyridin-2-ylmethyl)-carbamic acid benzyl ester 
• 159104-36-6 (3RS)-4-(Isopropenyloxycarbonyl)-3,6-dimethyl-3,4-dihydro-1,4,5-triazanaphthalen-2(1H)-one 

Relevant academic research and scientific papers

Pyridone or pyrimidinone derivatives as well as preparation method and application thereof

The present invention relates to pyridone or pyrimidinone derivatives. The invention discloses a preparation method and application thereof in medicine. , The present invention relates to a pyridone or pyrimidinone derivative represented by general formula (I), a preparation method thereof and a pharmaceutically acceptable salt thereof and as a therapeutic agent, in particular as a coagulation factor XIa (FXIa) inhibitor, wherein the definition of each substituent in the general formula (I) is the same as defined in the specification.

Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria

The discovery and development of new antibiotics capable of curing infections due to multidrug-resistant and pandrug-resistant Gram-negative bacteria are a major challenge with fundamental importance to our global healthcare system. Part of our broad program at Novartis to address this urgent, unmet need includes the search for new agents that inhibit novel bacterial targets. Here we report the discovery and hit-to-lead optimization of new inhibitors of phosphopantetheine adenylyltransferase (PPAT) from Gram-negative bacteria. Utilizing a fragment-based screening approach, we discovered a number of unique scaffolds capable of interacting with the pantetheine site of E. coli PPAT and inhibiting enzymatic activity, including triazolopyrimidinone 6. Structure-based optimization resulted in the identification of two lead compounds as selective, small molecule inhibitors of bacterial PPAT: triazolopyrimidinone 53 and azabenzimidazole 54 efficiently inhibited E. coli and P. aeruginosa PPAT and displayed modest cellular potency against the efflux-deficient E. coli ΔtolC mutant strain.

Discovery and Optimization of Phosphopantetheine Adenylyltransferase Inhibitors with Gram-Negative Antibacterial Activity

In the preceding manuscript [Moreau et al. 2018, 10.1021/acs.jmedchem.7b01691] we described a successful fragment-based lead discovery (FBLD) strategy for discovery of bacterial phosphopantetheine adenylyltransferase inhibitors (PPAT, CoaD). Following several rounds of optimization two promising lead compounds were identified: triazolopyrimidinone 3 and 4-azabenzimidazole 4. Here we disclose our efforts to further optimize these two leads for on-target potency and Gram-negative cellular activity. Enabled by a robust X-ray crystallography system, our structure-based inhibitor design approach delivered compounds with biochemical potencies 4-5 orders of magnitude greater than their respective fragment starting points. Additional optimization was guided by observations on bacterial permeability and physicochemical properties, which ultimately led to the identification of PPAT inhibitors with cellular activity against wild-type E. coli.

Lithium Hexamethyldisilazane Transformation of Transiently Protected 4-Aza/Benzimidazole Nitriles to Amidines and their Dimethyl Sulfoxide Mediated Imidazole Ring Formation

Trimethylsilyl-transient protection successfully allowed the use of lithium hexamethyldisilazane to prepare benzimidazole (BI) and 4-azabenzimidazole (azaBI) amidines from nitriles in 58-88% yields. This strategy offers a much better choice to prepare BI/azaBI amidines than the lengthy, low-yielding Pinner reaction. Synthesis of aza/benzimidazole rings from aromatic diamines and aldehydes was affected in dimethyl sulfoxide in 10-15 min, while known procedures require long time and purification. These methods are important for the BI/azaBI-based drug industry and for developing specific DNA binders for expanded therapeutic applications.

HETEROARYL COMPOUNDS AND USES THEREOF

The present invention relates to compounds useful as inhibitors of protein kinases, containing a cysteine residue in the ATP binding site. The invention further provides for pharmaceutically acceptable compositions comprising therapeutically effective amounts of one or more of the protein kinase inhibitor compounds and methods of using said compositions in the treatment of cancers and carcinomas.

4-METHYL-2,3,5,9,9B-PENTAAZA-CYCLOPENTA[A]NAPHTHALENES

The invention relates to 4-methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalene derivatives of general formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes

The invention relates to 4-methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalene derivatives of general formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

Mild and highly selective palladium-catalyzed monoarylation of ammonia enabled by the use of bulky biarylphosphine ligands and palladacycle precatalysts

A method for the Pd-catalyzed arylation of ammonia with a wide range of aryl and heteroaryl halides, including challenging five-membered heterocyclic substrates, is described. Excellent selectivity for monoarylation of ammonia to primary arylamines was achieved under mild conditions or at rt by the use of bulky biarylphosphine ligands (L6, L7, and L4) as well as their corresponding aminobiphenyl palladacycle precatalysts (3a, 3b, and 3c). As this process requires neither the use of a glovebox nor high pressures of ammonia, it should be widely applicable.

SUBSTITUTED DIAZEPINE SULFONAMIDES AS BOMBESIN RECEPTOR SUBTYPE-3 MODULATORS

Certain novel substituted diazepine sulfonamides are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.

SUBSTITUTED AMINOPYRIDINES AND USES THEREOF

This invention relates to novel compounds having the structural formula (I) and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.